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2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基] | 761440-16-8

物质功能分类

医药中间体 - 原料药中间体

分子结构分类

有机化合物 - 苯类化合物 - 苯和取代衍生物

中文名称

2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基]

中文别名

4-氨基嘧啶,2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基]-；2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基]-4-氨基嘧啶；2,5-二氯-N-[2-[(1-甲基乙基)磺酰基]苯基]-4-嘧啶胺；色瑞替尼中间体；2,5-二氯-N-(2-((1-甲基乙基)磺酰基)苯基)-4-嘧啶胺；4-氨基嘧啶, 2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基]-

英文名称

2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine

英文别名

2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidine-4-amine；2,5-dichloro-N-[2-(propane-2-sulfonyl)phenyl]pyrimidin-4-amine；2,5-dichloro-N-[2-[(1-methylethyl)sulfonyl]phenyl]pyrimidin-4-amine；2,5-dichloro-N-(2-((1-methylethyl)sulfonyl)phenyl)-4-pyrimidinamine；2,5‐dichloro‐N‐[2‐(isopropylsulfonyl)phenyl]pyrimidin‐4‐amine；2,5-dichloro-N-(2-propan-2-ylsulfonylphenyl)pyrimidin-4-amine

CAS

761440-16-8

化学式

C₁₃H₁₃Cl₂N₃O₂S

mdl

——

分子量

346.237

InChiKey

WWVLDJAVSQZSKO-UHFFFAOYSA-N

BEILSTEIN

——

EINECS

——

物化性质

熔点：

149.0 to 153.0 °C
沸点：

538℃
密度：

1.436
闪点：

279℃

计算性质

辛醇/水分配系数(LogP)：

4.3
重原子数：

21
可旋转键数：

4
环数：

2.0
sp3杂化的碳原子比例：

0.23
拓扑面积：

80.3
氢给体数：

1
氢受体数：

5

安全信息

海关编码：

2933599090
危险性防范说明：

P261,P280,P305+P351+P338
危险性描述：

H302+H312+H332,H315,H319,H335
储存条件：

2-8°C

SDS

SDS：586bf72355cec0d34ccb0aaa22981caa

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制备方法与用途

应用

2,5-二氯-N-[2-[(1-甲基乙基)磺酰基]苯基]-4-嘧啶胺是有机合成中间体和医药中间体，可用于实验室有机合成过程和化工医药研发过程中，主要用于合成原料药色瑞替尼。

用途：作为色瑞替尼的中间体。

上下游信息

上游原料

中文名称	英文名称	CAS号	化学式	分子量
——	2-hydroxy-5-chloro-N-[2-[(1-methylethyl)sulfonyl]phenyl]-4-pyrimidinamine	——	C₁₃H₁₄ClN₃O₃S	327.791

下游产品

中文名称	英文名称	CAS号	化学式	分子量
——	5-chloro-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1022961-58-5	C₁₃H₁₅ClN₄O₂S	326.807
——	(E)-2-(2-benzylidenehydrazinyl)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₀H₂₀ClN₅O₂S	429.93
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(pyridin-4-ylmethylene)hydrazinyl)pyrimidin-4-amine	——	C₁₉H₁₉ClN₆O₂S	430.918
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(4-(methylthio)benzylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₁H₂₂ClN₅O₂S₂	476.023
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(pyridin-3-ylmethylene)hydrazinyl)pyrimidin-4-amine	——	C₁₉H₁₉ClN₆O₂S	430.918
——	(E)-5-chloro-2-(2-(2-chlorobenzylidene)hydrazinyl)-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₀H₁₉Cl₂N₅O₂S	464.375
——	(E)-5-chloro-2-(2-(2-fluorobenzylidene)hydrazinyl)-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₀H₁₉ClFN₅O₂S	447.921
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(4-methoxybenzylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₁H₂₂ClN₅O₃S	459.956
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(1-(p-tolyl)ethylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₂H₂₄ClN₅O₂S	457.984
——	2-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)acetamide	——	C₂₁H₂₃ClN₆O₃S	474.971
——	3-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)propanamide	——	C₂₂H₂₅ClN₆O₃S	488.998
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(1-(4-(methylthio)phenyl)ethylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₂H₂₄ClN₅O₂S₂	490.05
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(4-nitrobenzylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₀H₁₉ClN₆O₄S	474.928
——	(E)-4-(1-(2-(5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)hydrazono)ethyl)benzonitrile	——	C₂₂H₂₁ClN₆O₂S	468.967
——	(E)-2-(2-(1-(4-bromophenyl)ethylidene)hydrazinyl)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₁H₂₁BrClN₅O₂S	522.853
——	4-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)butanamide	——	C₂₃H₂₇ClN₆O₃S	503.025
——	(E)-5-chloro-2-(2-(2,4-difluorobenzylidene)hydrazinyl)-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₀H₁₈ClF₂N₅O₂S	465.911
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(3-methoxybenzylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₁H₂₂ClN₅O₃S	459.956
——	(E)-5-chloro-2-(2-(1-(4-fluorophenyl)ethylidene)hydrazinyl)-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₁H₂₁ClFN₅O₂S	461.947
——	(S)-2-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)propanamide	——	C₂₂H₂₅ClN₆O₃S	488.998
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(2-methoxybenzylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₁H₂₂ClN₅O₃S	459.956
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)azetidine-3-carboxamide	——	C₂₃H₂₅ClN₆O₃S	501.009
——	(E)-5-chloro-N-(2-(isopropylsulfonyl)phenyl)-2-(2-(1-(4-methoxyphenyl)ethylidene)hydrazinyl)pyrimidin-4-amine	——	C₂₂H₂₄ClN₅O₃S	473.983
——	2-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-methylpropanamide	——	C₂₃H₂₇ClN₆O₃S	503.025
——	(S)-2-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-3-methylbutanamide	——	C₂₄H₂₉ClN₆O₃S	517.052
——	(E)-5-chloro-2-(2-(1-(2-fluorophenyl)ethylidene)hydrazinyl)-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₁H₂₁ClFN₅O₂S	461.947
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(piperazin-1-yl)acetamide	——	C₂₅H₃₀ClN₇O₃S	544.077
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(4-methylpiperazin-1-yl)acetamide	——	C₂₆H₃₂ClN₇O₃S	558.104
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-morpholinoacetamide	——	C₂₅H₂₉ClN₆O₄S	545.062
——	1-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)cyclopropanecarboxamide	——	C₂₃H₂₅ClN₆O₃S	501.009
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)azetidine-2-carboxamide	——	C₂₃H₂₅ClN₆O₃S	501.009
——	(E)-5-chloro-2-(2-(1-(2,4-difluorophenyl)ethylidene)hydrazinyl)-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine	——	C₂₁H₂₀ClF₂N₅O₂S	479.938
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)-amino)pyrimidin-2-yl)amino)phenyl)-2-(4-(oxetan-3-yl)piperazin-1-yl)acetamide	——	C₂₈H₃₄ClN₇O₄S	600.141
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(4-(2-hydroxyacetyl)piperazin-1-yl)acetamide	——	C₂₇H₃₂ClN₇O₅S	602.114
——	5-chloro-N⁴-(2-(isopropylsulfonyl) phenyl)-N2-(2-methoxy-4-nitrophenyl) pyrimidine-2,4-diamine	——	C₂₀H₂₀ClN₅O₅S	477.928
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)acetamide	——	C₂₇H₃₂ClN₇O₃S	570.115
——	5-chloro-N2-(3,5-dimethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1564256-44-5	C₂₅H₃₀ClN₅O₂S	500.064
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(furan-2-yl)acetamide	——	C₂₅H₂₄ClN₅O₄S	526.016
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-((2S,6R)-2,6-dimethylmorpholino)acetamide	——	C₂₇H₃₃ClN₆O₄S	573.116
——	2-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino) pyrimidin-2-yl)amino)thiazole-4-carboxylic acid	——	C₁₇H₁₆ClN₅O₄S₂	453.93
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)-amino)pyrimidin-2-yl)amino)phenyl)-1-(4-(dimethylamino)butanoyl)azetidine-3-carboxamide	——	C₂₉H₃₆ClN₇O₄S	614.168
——	(E)-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)-amino)pyrimidin-2-yl)amino)phenyl)-2-(4-(4-(dimethylamino)but-2-enoyl)piperazin-1-yl)acetamide	——	C₃₁H₃₉ClN₈O₄S	655.221
——	2-(2,5-diazabicyclo[2.2.1]heptan-2-yl)-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)acetamide	——	C₂₆H₃₀ClN₇O₃S	556.088
——	2-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-methoxy-2-methylphenyl)acetonitrile	——	C₂₃H₂₄ClN₅O₃S	485.994
——	2-ethoxyethyl 2-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidine-2-yl)amino)-4-methoxyphenyl)acetate	——	C₂₆H₃₁ClN₄O₆S	563.074
——	5-chloro-N²-[4-(dimethylphosphoryl)-2-methoxyphenyl]-N⁴-[2-(propan-2-ylsulfonyl)phenyl]pyrimidine-2,4-diamine	——	C₂₂H₂₆ClN₄O₄PS	508.966
——	2-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)acetamide	——	C₂₇H₃₁ClN₆O₄S	571.1
——	(S)-2-amino-N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-3-(1H-imidazol-4-yl)propanamide	——	C₂₅H₂₇ClN₈O₃S	555.06
——	5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-5-methyl-4-(2-(methylamino)ethyl)phenyl)pyrimidine-2,4-diamine	——	C₂₄H₃₀ClN₅O₃S	504.053
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(hexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl)acetamide	——	C₂₇H₃₂ClN₇O₃S	570.115
5-氯-N2-(2-异丙氧基-4-(哌啶-4-基)苯基)-N4-(2-(异丙基磺酰基)苯基)嘧啶-2,4-二胺	5-chloro-N2-(2-isopropoxy-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1032903-33-5	C₂₇H₃₄ClN₅O₃S	544.118
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl)acetamide	——	C₂₇H₃₁ClN₆O₄S	571.1
——	5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(8-methoxy-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)pyrimidine-2,4-diamine	——	C₂₄H₂₈ClN₅O₃S	502.037
——	N-(3-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)-2-(1H-indol-2-yl)acetamide	——	C₂₉H₂₇ClN₆O₃S	575.091
——	5-chloro-N⁴-(2-(isopropylsulfonyl)phenyl)-N²-(6-methoxy-1,2,3,4-tetrahydroisoquinolin-7-yl)pyrimidine-2,4-diamine	——	C₂₃H₂₆ClN₅O₃S	488.01
——	5-chloro-N4-((2-((isopropylsulfonyl)phenylamino)pyrimidin-2-yl)amino-N2-8-methoxy-4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)ethanol	1022949-63-8	C₂₆H₃₂ClN₅O₄S	546.09
——	5-chloro-N2-(4-isopropoxy-2-(piperidin-4-yl)pyrimidin-5-yl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1032903-43-7	C₂₅H₃₂ClN₇O₃S	546.093
——	N2-(5-amino-4-(4-ethylpiperazin-1-yl)-2-methoxyphenyl)-5-chloro-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	——	C₂₆H₃₄ClN₇O₃S	560.12
——	5-chloro-N2-(2-isopropoxy-5-methyl-4-morpholin-4-ylmethyl-phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine	1032900-23-4	C₂₈H₃₆ClN₅O₄S	574.144
——	5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(7-methoxy-2,3,4,5-tetrahydro-1H-benzo[c]azepin-8-yl)pyrimidine-2,4-diamine	——	C₂₄H₂₈ClN₅O₃S	502.037
——	(2-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)thiazol-4-yl) (piperidin-1-yl)methanone	——	C₂₂H₂₅ClN₆O₃S₂	521.064
色瑞替尼	ceritinib	1032900-25-6	C₂₈H₃₆ClN₅O₃S	558.145
——	5-chloro-N⁴-(2-(isopropylsulfonyl)phenyl)-N²-(5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-yl)pyrimidine-2,4-diamine	——	C₂₀H₂₃ClN₆O₂S₂	479.027
——	2-(7-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-6-methoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-ol	——	C₂₅H₃₀ClN₅O₄S	532.063
——	5-chloro-N2-(2-isopropoxy-5-methyl-4-(1-ethylpiperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1445895-03-3	C₃₀H₄₀ClN₅O₃S	586.198
——	5-chloro-N2-(2-cyclobutoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1032901-06-6	C₂₉H₃₆ClN₅O₃S	570.156
——	5-chloro-N²-(2-(2-(dimethylamino)ethyl)-6-methoxy-1,2,3,4-tetrahydroisoquinolin-7-yl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	——	C₂₇H₃₅ClN₆O₃S	559.132
——	8-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5,9-dimethoxyphenanthridin-6(5H)-one	——	C₂₈H₂₆ClN₅O₅S	580.064
——	5-chloro-N2-(2-isopropoxy-5-methyl-4-(1-isopropylpiperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1445895-04-4	C₃₁H₄₂ClN₅O₃S	600.225
——	5-chloro-N²-((prop-2-yloxy)-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	——	C₂₈H₃₆ClN₅O₃S	559.137
——	5-chloro-N2-(4-(1-(2,2-difluoroethyl)piperidin-4-yl)-2-isopropoxy-5-methylphenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	1445895-08-8	C₃₀H₃₈ClF₂N₅O₃S	622.179
——	1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-3-(2-morpholinoethyl)imidazolidin-2-one	——	C₂₉H₃₆ClN₇O₅S	630.168
——	1-(7-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-6-methoxy-3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxyethan-1-one	——	C₂₅H₂₈ClN₅O₅S	546.047
——	N-(5-(5-chloro-4-(2-(isopropylsulfonyl)phenylamino)pyrimidin-2-ylamino)-2-(4-ethylpiperazin-1-yl)-4-methoxyphenyl)acrylamide	——	C₂₉H₃₆ClN₇O₄S	614.168
——	1-(4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidin-1-yl)-2-(dimethylamino)ethanone	1190399-47-3	C₃₂H₄₃ClN₆O₄S	643.25
——	7-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-N-ethyl-6-methoxy-3,4-dihydroisoquinoline-2(1H)-carboxamide	——	C₂₆H₃₁ClN₆O₄S	559.089
——	1-(2-{5-chloro-4-[2-(propane-2-sulfonyl)phenylamino]-2-ylamino}-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-6-yl)-2-hydroxy-ethanone	——	C₂₂H₂₅ClN₆O₄S₂	537.063
——	methyl 4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate	——	C₃₀H₃₈ClN₅O₅S	616.181
——	ethyl 4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate	——	C₃₁H₄₀ClN₅O₅S	630.208
——	(R)-1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-3-(oxiran-2-ylmethyl)imidazolidin-2-one	——	C₂₆H₂₉ClN₆O₅S	573.072
——	6-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-7-methoxy-1,1-dimethyl-3,4-dihydronaphthalen-2(1H)-one	——	C₂₆H₂₉ClN₄O₄S	529.06
4-(4-((5-氯-4-((2-((丙烷-2-基)磺酰基)苯基)氨基)嘧啶-2-基)氨基)-5-异丙氧基-2-甲基苯基)哌啶-1-羧酸叔丁酯	4-(4-{5-chloro-4-[2-(propane-2-sulfonyl)phenylamino]pyrimidin-2-ylamino}-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylic acid tert-butyl ester	1032903-64-2	C₃₃H₄₄ClN₅O₅S	658.262
——	7-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-6-methoxy-1,1-dimethyl-3,4-dihydronaphthalen-2(1H)-one	——	C₂₆H₂₉ClN₄O₄S	529.06
——	N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide	——	C₂₉H₃₆ClN₇O₄S	614.168
——	1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-3-(2-(3-hydroxyazetidin-1-yl)-2-oxoethyl)imidazolidin-2-one	——	C₂₈H₃₂ClN₇O₆S	630.124
——	sec-butyl 4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate	——	C₃₃H₄₄ClN₅O₅S	658.262
——	1-(4-((1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)ethan-1-one	——	C₂₉H₃₄ClN₉O₄S	640.166
——	3-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-N,N-dimethyl-2-oxoimidazolidine-1-amide	——	C₂₆H₃₀ClN₇O₅S	588.087
——	1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)-3-(2-oxo-2-thiomorpholinoethyl)imidazolidin-2-one	——	C₂₉H₃₄ClN₇O₅S₂	660.2
——	N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-2-(4-cyc lohexylpiperazin-1-yl)-4-methoxyphenyl)acrylamide	——	C₃₃H₄₂ClN₇O₄S	668.26
——	pentyl 4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate	——	C₃₄H₄₆ClN₅O₅S	672.289
——	2-(4-((2-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-isopropoxyphenyl)thiazol-4-yl)methyl)piperazin-1-yl)ethan-1-ol	——	C₃₂H₄₀ClN₇O₄S₂	686.299
——	5-chloro-N²-(2-(d₇-isopropoxy)-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	——	C₂₈H₃₆ClN₅O₃S	565.089
——	acetoxymethyl 4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate	——	C₃₂H₄₀ClN₅O₇S	674.218
——	5-chloro-N²-(2-isopropoxy-5-methyl-4-(2,2,6,6-d₄-piperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	——	C₂₈H₃₆ClN₅O₃S	562.113
——	(phosphonooxy)methyl 4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate	——	C₃₀H₃₉ClN₅O₉PS	712.161
——	5-chloro-N²-(2-(2-d-prop-2-yloxyl)-5-methyl-4-(2,2,6,6-tetrafluoropiperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine	——	C₂₈H₃₆ClN₅O₃S	563.105
——	6-{5-chloro-4-[2-(propane-2-sulfonyl)-phenylamino]-pyrimidin-2-ylamino}-5-isopropoxy-2-piperidin-4-yl-2,3-dihydro-isoindol-1-one	1032900-18-7	C₂₉H₃₅ClN₆O₄S	599.154
——	diethyl (4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidin-1-yl)phosphonate	——	C₃₂H₄₅ClN₅O₆PS	694.232
——	1-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-mehoxyphenyl)-3-(tetrahydro-2H-pyran-4-carbonyl)imidazol-2-one	——	C₂₉H₃₃ClN₆O₆S	629.137

反应信息

作为反应物：

描述：

2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基] 在二(三叔丁基膦)钯、碳酸氢钠、三氟乙酸、 sodium t-butanolate 作用下，以二氯甲烷、水、乙酸乙酯、甲苯为溶剂，反应 1.33h，生成色瑞替尼

参考文献：

名称：

신규 키나아제 억제제

摘要：

本发明是关于一种作为肿瘤、神经及精神疾病治疗药物的有用的新型キナラジン抑制剂的技术。

公开号：

KR20160147358A
作为产物：

描述：

2-(异丙基磺酰基)苯胺在 sodium hydride 、溶剂黄146 、三氯氧磷作用下，以水、 N,N-二甲基甲酰胺、甲苯为溶剂，反应 3.0h，生成 2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基]

参考文献：

名称：

色瑞替尼中间体及其制备方法

摘要：

本发明公开了一种色瑞替尼中间体及其制备方法。本发明的色瑞替尼中间体的制备方法包括如下步骤：(1)在无水无氧条件下，在极性非质子溶剂中，在金属氢化物存在的条件下，将中间体V与IV进行N‑芳基化反应，制得中间体III；(2)在溶剂中，酸性条件下，将所述的中间体III水解，制得中间体II；(3)在溶剂中，将所述的中间体II进行氯代反应，即可。本发明的制备方法所使用的原料安全无毒、反应简单易操作，副反应少，采用水进行后处理甚至是结晶，降低了生产成本，制得的产品纯度高，易于工业化大生产。

公开号：

CN107602483B
作为试剂：

描述：

2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基] 、 4-(4-氨基-5-异丙氧基-2-甲基苯基)哌啶-1-羧酸叔丁酯在 2,5-二氯-N-[2-[(1-甲基乙基)磺酰]苯基] 作用下，以39的产率得到色瑞替尼

参考文献：

名称：

一种色瑞替尼的制备方法

摘要：

本发明公开了一种色瑞替尼的制备方法，属于化学制药领域，以3-溴-4-甲基苯酚为起始原料经过酚羟基异丙基化、硝化、偶联、还原反应得到中间体1，再以邻硝基氟苯为另一起始原料经异巯基化、氧化、还原、嘧啶化得中间体2，1与2偶联反应得BOC酸酐保护的色瑞替尼，最后脱除叔丁氧羰基保护基得到色瑞替尼。本发明是一种操作简单易行，收率比较高，污染小，适合工业化生产的方法。

公开号：

CN104356112A

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文献信息

[EN] COMPOUNDS THAT MODULATE EGFR ACTIVITY AND METHODS FOR TREATING OR PREVENTING CONDITIONS THEREWITH<br/>[FR] COMPOSÉS MODULANT L'ACTIVITÉ DES RÉCEPTEURS EGFR ET MÉTHODES POUR TRAITER OU PRÉVENIR DES TROUBLES À L'AIDE DE CEUX-CI

申请人：GATEKEEPER PHARMACEUTICALS INC

公开号：WO2011140338A1

公开（公告）日：2011-11-10

Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.

提供了用于治疗或预防激酶介导的疾病的化合物和方法。
Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors

申请人：Buschmann Nicole

公开号：US20150119385A1

公开（公告）日：2015-04-30

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

本发明提供了化合物(I)或其药学上可接受的盐；制造该化合物的方法及其治疗用途。本发明还提供了药理活性剂的组合物和包括该化合物的药物组合。
[EN] RING-FUSED BICYCLIC PYRIDYL DERIVATIVES AS FGFR4 INHIBITORS<br/>[FR] DÉRIVÉS PYRIDYLE BICYCLIQUES À ANNEAUX FUSIONNÉS UTILISÉS EN TANT QU'INHIBITEURS DE FGFR4

申请人：NOVARTIS AG

公开号：WO2015059668A1

公开（公告）日：2015-04-30

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

本发明提供了化合物(I)或其药学上可接受的盐；制备该化合物的方法及其治疗用途。本发明还提供了药理活性剂的组合物和包含该化合物的药物组合物。
N2-(2-METHOXYPHENYL)PYRIMIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION FOR CANCER PREVENTION OR TREATMENT CONTAINING SAME AS ACTIVE INGREDIENT

申请人：KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

公开号：US20180111905A1

公开（公告）日：2018-04-26

The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.

本发明涉及一种N2-(2-甲氧基苯基)嘧啶衍生物，其制备方法，以及包含其作为活性成分的用于预防或治疗癌症的药物组合物。本发明的N2-(2-甲氧基苯基)嘧啶衍生物，其光学异构体，或其药学上可接受的盐对抑制间变性淋巴瘤激酶（ALK）活性非常有效，从而可以提高对具有间变性淋巴瘤激酶（ALK）融合蛋白如EML4-ALK和NPM-ALK的癌细胞的治疗效果，因此可以有效地用作预防或治疗癌症的药物组合物。
Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1

作者：Yu Wang、Guogang Zhang、Gang Hu、Yanxin Bu、Hongrui Lei、Daiying Zuo、Mengting Han、Xin Zhai、Ping Gong

DOI：10.1016/j.ejmech.2016.06.056

日期：2016.11

A series of 4-arylaminopyrimidine derivatives possessing a hydrazone moiety were designed, synthesized and evaluated for their biological activity. Most compounds exhibited moderate to excellent cytotoxic activity against ALK-addicted KARPAS299 and ROS1-addicted HCC78, while also showing much less potent activity against A549, H460 and HT-29, whose growth were not dependent on ALK and/or ROS1, as compared

设计，合成并评估了一系列具有部分的4-芳基氨基嘧啶衍生物，并对其生物学活性进行了评估。大多数化合物对ALK上瘾的KARPAS299和ROS1上瘾的HCC78表现出中等至优异的细胞毒活性，而与A549，H460和HT-29相比，它们的生长活性要弱得多，而A549，H460和HT-29的生长不依赖于ALK和/或ROS1。克唑替尼和塞立替尼。最有希望的化合物7b对ALK上瘾的KARPAS299和ROS1上瘾的HCC78细胞系显示出高抗增殖作用，IC 50分别为20 nM和28 nM，但对A549，H460和HT-29没有抑制活性。酶法鉴定7b作为有效和选择性的ALK和ROS1双重抑制剂，IC 50分别为2.5 nM和2.7 nM。它还对L1196M ALK表现出良好的抑制活性，IC 50值为67 nM。