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4-(3-氯-4-氟苯胺)-7-甲氧基-喹唑啉-6-醇 | 184475-71-6

物质功能分类

有机原料 - 有机氟化合物 - 氟苯胺系列

分子结构分类

有机化合物 - 有机杂环化合物 - 二氮杂萘

中文名称

4-(3-氯-4-氟苯胺)-7-甲氧基-喹唑啉-6-醇

中文别名

4-(3-氯-4-氟苯胺)-6-羟基-7-甲氧基喹唑啉；吉非替尼中间体7；氧位O-去丙基吗啉吉非替尼；4-(3-氯-4-氟苯氨基)-7-甲氧基喹唑啉-6-醇；4-(3-氯-4-氟苯)氨基-7-甲氧基-6-羟基喹唑啉；4-(3-氯-4-氟苯胺)-7-甲氧基-6-羟基喹唑啉；4-(3-氯-4-氟苯胺基)-7-甲氧基-6-羟基喹唑啉；(2)6-(甲氧基)-7-苄氧基喹唑啉-4-酮

英文名称

4-(3-chloro-4-fluorophenylamino)-6-hydroxy-7-methoxyquinazoline

英文别名

4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol；4-(3-chloro-4-fluoroanilino)-6-hydroxy-7-methoxyquinazoline；O-desmorpholinopropyl gefitinib；dMG；4-(3′-chloro-4′-fluoroanilino)-6-hydroxy-7-methoxyquinazoline；4-(3-chloro-4-fluoroaniline)-7-methoxyquinazolin-6-ol；4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-ol；4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-ol

CAS

184475-71-6

化学式

C₁₅H₁₁ClFN₃O₂

mdl

——

分子量

319.723

InChiKey

JLVTVCRXFMLUIF-UHFFFAOYSA-N

BEILSTEIN

——

EINECS

——

物化性质

熔点：

>260°C (dec.)
沸点：

478.8±45.0 °C(Predicted)
密度：

1.489±0.06 g/cm3(Predicted)
溶解度：

可溶于DMSO（轻微）、甲醇（非常轻微，加热）

计算性质

辛醇/水分配系数(LogP)：

3.8
重原子数：

22
可旋转键数：

3
环数：

3.0
sp3杂化的碳原子比例：

0.07
拓扑面积：

67.3
氢给体数：

2
氢受体数：

6

安全信息

海关编码：

2933990090
危险性防范说明：

P261,P305+P351+P338
危险性描述：

H302,H315,H319,H335
储存条件：

存储温度建议在0至10℃之间，并请避免加热。

SDS

SDS：aba1ed95e0821a5ca4d4ef0112b0b6ad

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制备方法与用途

生物活性方面，FAAH-IN-2（O-脱吗啡基丙基吉非替尼）是一种源自专利WO/2008/100977A2的FAAH抑制剂。其主要用途为吉非替尼中间体。

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
——	N-(3-chloro-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine	——	C₁₆H₁₃ClFN₃O₂	333.75
4-(3-氯-4-氟苯氨基)-7-甲氧基喹唑啉-6-醇乙酸酯	4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl acetate	788136-89-0	C₁₇H₁₃ClFN₃O₃	361.76
N-(3-氯-4-氟苯基)-7-甲氧基-6-苄氧基喹唑啉-4-胺	6-(benzyloxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine	913819-12-2	C₂₂H₁₇ClFN₃O₂	409.847

下游产品

中文名称	英文名称	CAS号	化学式	分子量
——	2-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)ethan-1-ol	905306-09-4	C₁₇H₁₅ClFN₃O₃	363.776
——	4-(3-chloro-4-fluorophenylamino)-6-(2-chloroethoxy)-7-methoxyquinazoline	808793-73-9	C₁₇H₁₄Cl₂FN₃O₂	382.221
——	N-(3-chloro-4-fluorophenyl)-6-(2-fluoroethoxy)-7-methoxyquinazolin-4-amine	1389355-13-8	C₁₇H₁₄ClF₂N₃O₂	365.767
——	N-(3-chloro-4-fluorophenyl)-6-(2-[18F]fluoroethoxy)-7-methoxyquinazolin-4-amine	1389355-28-5	C₁₇H₁₄ClF₂N₃O₂	364.768
——	4-(3'-chloro-4'-fluoroanilino)-6-(prop-2-ynyloxy)-7-methoxyquinazoline	1214731-77-7	C₁₈H₁₃ClFN₃O₂	357.772
——	4-(3'-chloro-4'-fluoroanilino)-6-(2-bromoethoxy)-7-methoxyquinazoline	——	C₁₇H₁₄BrClFN₃O₂	426.672
——	(6-allyloxy-7-methoxy-quinazolin-4-yl)-(3-chloro-4-fluoro-phenyl)-amine	——	C₁₈H₁₅ClFN₃O₂	359.787
——	4-(3-chloro-4-fluoro)phenylamino-6-aminoethoxy-7-methoxyquinazoline	1428015-62-6	C₁₇H₁₆ClFN₄O₂	362.791
——	2-[4-(3-Chloro-4-fluoroanilino)-7-(2-hydroxyethoxy)quinazolin-6-yl]oxyethanol	1373944-89-8	C₁₈H₁₇ClFN₃O₄	393.802
——	3-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propan-1-ol	1221965-74-7	C₁₈H₁₇ClFN₃O₃	377.803
——	6,7-bis(2-bromoethoxy)-N-(3-chloro-4-fluorophenyl)quinazolin-4-amine	1373944-93-4	C₁₈H₁₅Br₂ClFN₃O₂	519.595
——	6,7-bis(2-aminoethoxy)-N-(3-chloro-4-fluorophenyl)quinazolin-4-amine	1373944-97-8	C₁₈H₁₉ClFN₅O₂	391.833
——	6-(3-aminopropoxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine	655247-75-9	C₁₈H₁₈ClFN₄O₂	376.818
吉非替尼中间体B	N-(3-chloro-4-fluorophenyl)-6-(3-chloropropoxy)-7-methoxyquinazolin-4-amine	912556-91-3	C₁₈H₁₆Cl₂FN₃O₂	396.248
——	6-(3-bromopropoxy)-4-(3'-chloro-4'-fluoroanilino)-7-methoxyquinazoline	——	C₁₈H₁₆BrClFN₃O₂	440.699
——	4-(3-chloro-4-fluorophenylamino)-6-hexyloxy-7-methoxyquinazoline	1214731-90-4	C₂₁H₂₃ClFN₃O₂	403.884
——	6-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)hexan-1-ol	1012057-92-9	C₂₁H₂₃ClFN₃O₃	419.883
——	4-(3'-chloro-4'-fluorophenylamino)-6-(hex-5-enyloxy)-7-methoxyquinazoline	1214731-89-1	C₂₁H₂₁ClFN₃O₂	401.868
——	4-(3'-chloro-4'-fluoroanilino)-6-(2-dimethylaminoethoxy)-7-methoxyquinazoline	——	C₁₉H₂₀ClFN₄O₂	390.845
——	4-(3'-chloro-4'-fluoroanilino)-6-(2-(2-aminoethyl)aminoethoxy)-7-methoxyquinazoline	1360859-35-3	C₁₉H₂₁ClFN₅O₂	405.859
——	4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(pent-4-ynyloxy)quinazoline	1214731-79-9	C₂₀H₁₇ClFN₃O₂	385.825
——	4-(3'-chloro-4'-fluoroanilino)-6-(hex-5-ynyloxy)-7-methoxyquinazoline	1214731-80-2	C₂₁H₁₉ClFN₃O₂	399.852
——	4-(3'-chloro-4'-fluoroanilino)-6-(hept-6-ynyloxy)-7-methoxyquinazoline	1214731-81-3	C₂₂H₂₁ClFN₃O₂	413.879
——	4-(3'-chloro-4'-fluoroanilino)-6-(3-dimethylaminopropoxy)-7-methoxyquinazoline	——	C₂₀H₂₂ClFN₄O₂	404.872
——	2-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)acetic acid	1373944-75-2	C₁₇H₁₃ClFN₃O₄	377.759
——	4-(3-chloro-4-fluoroanilino)-6-(N-(2-aminoethyl)aminopropoxy)-7-methoxyquinazoline	1373944-38-7	C₂₀H₂₃ClFN₅O₂	419.886
——	4-(3'-chloro-4'-fluoroanilino)-6-(2-diethylaminoethoxy)-7-methoxyquinazoline	——	C₂₁H₂₄ClFN₄O₂	418.899
——	4-(3'-chloro-4'-fluoroanilino)-6-(3-diethylaminopropoxy)-7-methoxyquinazoline	——	C₂₂H₂₆ClFN₄O₂	432.925
——	methyl 3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propanote	1214998-19-2	C₁₉H₁₇ClFN₃O₄	405.813
2-(4-(3-氯-4-氟苯基氨基)-7-甲氧基喹唑啉-6-氧基)-N-羟基乙酰胺	2-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyacetamide	1012054-52-2	C₁₇H₁₄ClFN₄O₄	392.774
——	4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-piperidinopropoxy)-quinazoline	——	C₂₃H₂₆ClFN₄O₂	444.936
——	4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-pyrrolidin-1-ylpropoxy)-quinazoline	——	C₂₂H₂₄ClFN₄O₂	430.91
——	4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(3-methyloxetan-3-ylmethoxy)quinazoline	——	C₂₀H₁₉ClFN₃O₃	403.841
——	4-(3'-chloro-4'-fluoroanilino)-6-(1,3-dioxolan-2-ylmethoxy)-7-methoxyquinazoline	——	C₁₉H₁₇ClFN₃O₄	405.813
——	thyl 2-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)acetate	1012057-13-4	C₁₉H₁₇ClFN₃O₄	405.813
——	4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-(2-piperidinoethoxy)quinazoline	——	C₂₂H₂₄ClFN₄O₂	430.91
——	ethyl 4-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)butanoate	1012057-14-5	C₂₁H₂₁ClFN₃O₄	433.867
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine	295330-45-9	C₂₂H₂₅ClFN₅O₂	445.924
——	(3-chloro-4-fluorophenyl)-(7-methoxy-6-(3-(1,4,7-triazacyclononan-1-yl)propoxy)quinazolin-4-yl)amine	——	C₂₄H₃₀ClFN₆O₂	488.993
——	ethyl 4-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)pentanoate	——	C₂₂H₂₃ClFN₃O₄	447.894
吉非替尼	gefitinib	184475-35-2	C₂₂H₂₄ClFN₄O₃	446.909
——	ethyl 7-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)heptanoate	1012057-16-7	C₂₄H₂₇ClFN₃O₄	475.947
——	ethyl 6-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)hexanoate	1012057-15-6	C₂₃H₂₅ClFN₃O₄	461.921
——	4-(3'-chloro-4'-fluoroanilino)-6-(2-(1H-imidazol-1-yl)ethoxy)-7-methoxyquinazoline	——	C₂₀H₁₇ClFN₅O₂	413.839
——	4-(3'-chloro-4'-fluoroanilino)-6-(1,3-dioxolan-4-ylmethoxy)-7-methoxyquinazoline	——	C₁₉H₁₇ClFN₃O₄	405.813
——	tert-butyl (3-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)carbamate	——	C₂₃H₂₆ClFN₄O₄	476.935
——	6-(2-(3-(1H-imidazol-1-yl) propoxy))-4-(3′-chloro-4′-fluoroanilino)-7-methoxyquinazoline	——	C₂₁H₁₉ClFN₅O₂	427.866
——	4-(3'-chloro-4'-fluoroanilino)-7-methoxy-6-tetrahydrofuran-2-ylmethoxyquinazoline	——	C₂₀H₁₉ClFN₃O₃	403.841
——	4-(3-chloro-4-fluoroanilino)-7-methoxy-6-(pyridin-2-ylmethoxy)quinazoline	——	C₂₁H₁₆ClFN₄O₂	410.835
——	methyl 4-(2-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)ethoxy)benzoate	1012057-89-4	C₂₅H₂₁ClFN₃O₅	497.91
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438072-41-3	C₂₄H₂₇ClFN₅O₂	471.962
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(5-methylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)propoxy)quinazolin-4-amine	1438072-47-9	C₂₅H₂₉ClFN₅O₂	485.989
——	(E)-methyl 3-(4-(2-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)ethoxy)phenyl) acrylate	1012057-57-6	C₂₇H₂₃ClFN₃O₅	523.948
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(octahydroisoquinolin-2(1H)-yl)propoxy)quinazolin-4-amine	1438073-86-9	C₂₇H₃₂ClFN₄O₂	499.028
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(octahydro-2,7-naphthyridin-2(1H)-yl)propoxy)quinazolin-4-amine	1438073-74-5	C₂₆H₃₁ClFN₅O₂	500.016
——	4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)morpholin-2-one	——	C₂₂H₂₂ClFN₄O₄	460.892
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-yl)propoxy)quinazolin-4-amine	1438075-28-5	C₂₄H₂₆ClFN₄O₃	472.947
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydro-1H-pyrrolo[3,4-c]pyridin-2(3H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438073-56-3	C₂₅H₂₉ClFN₅O₂	485.989
——	4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoic acid	——	C₂₆H₂₉ClFN₅O₅	545.998
——	4-(3'-chloro-4'-fluorophenylamino)-6-[2-(2-oxa-6-azaspiro[3.4]octane-6-yl)oxethyl]-7-methoxyquinazoline	1445860-69-4	C₂₃H₂₄ClFN₄O₃	458.92
——	N-(3-chloro-4-fluorophenyl)-6-(3-(6-(dimethylamino)-3-azabicyclo[3.1.0]hexan-3-yl)propoxy)-7-methoxyquinazolin-4-amine	1438073-68-7	C₂₅H₂₉ClFN₅O₂	485.989
——	4-(3'-chloro-4'-fluorophenylamino)-7-methoxy-6-(trifluoromethanesulfonyloxy)quinazoline	451494-86-3	C₁₆H₁₀ClF₄N₃O₄S	451.786
——	4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl L-leucinate	——	C₂₁H₂₂ClFN₄O₃	432.882
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydrofuro[3,4-c]pyridin-5(3H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438073-98-3	C₂₅H₂₈ClFN₄O₃	486.974
——	methyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₂₇H₃₁ClFN₅O₅	560.025
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydro-1H-pyrrolo[3,2-c]pyridin-5(6H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438072-89-9	C₂₅H₂₉ClFN₅O₂	485.989
——	methyl 6-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-6-oxohexanoate	——	C₂₉H₃₅ClFN₅O₅	588.079
——	methyl 7-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-7-oxoheptanoate	——	C₃₀H₃₇ClFN₅O₅	602.106
——	methyl 8-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-8-oxooctanoate	——	C₃₁H₃₉ClFN₅O₅	616.133
——	methyl 9-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-9-oxononanoate	——	C₃₂H₄₁ClFN₅O₅	630.159
——	methyl 5-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-5-oxopentanoate	——	C₂₈H₃₃ClFN₅O₅	574.052
——	tert-butyl 4-[3-[4-(3-chloro-4-fluoro-anilino)-7-methoxy-quinazolin-6-yl]oxypropyl]piperazine-1-carboxylate	295330-38-0	C₂₇H₃₃ClFN₅O₄	546.042
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydropyrano[3,4-c]pyrrol-2(3H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438073-13-2	C₂₅H₂₈ClFN₄O₃	486.974
——	ethyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₂₈H₃₃ClFN₅O₅	574.052
——	propyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₂₉H₃₅ClFN₅O₅	588.079
——	butyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₀H₃₇ClFN₅O₅	602.106
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-((4aS,7aS)-tetrahydro-2H-[1,4]dioxino[2,3-c]pyrrol-6(3H)-yl)propoxy)quinazolin-4-amine	——	C₂₄H₂₆ClFN₄O₄	488.946
——	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(tetrahydro-2H-[1,4]dioxino[2,3-c]pyrrol-6(3H)-yl)propoxy)quinazolin-4-amine	1438075-40-1	C₂₄H₂₆ClFN₄O₄	488.946
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydro-1H-pyrrolo[2,3-c]pyridin-6(2H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438072-77-5	C₂₅H₂₉ClFN₅O₂	485.989
——	4-[(3-chloro-4-fluoro-phenyl)amino]-7-methoxy-6-{3-[(1R,6S)-2,5-dioxa-8-azabicyclo[4.3.0]nonane-8-yl]propoxy}-quinazoline	——	C₂₄H₂₆ClFN₄O₄	488.946
——	pentyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₁H₃₉ClFN₅O₅	616.133
——	3-((4-((3-chloro-4-fluorophenylamino))-7-methoxyquinazolin-6-yl)oxy)propyl N,N-bis(2-chloroethyl)phosphorodiamidate	——	C₂₂H₂₆Cl₃FN₅O₄P	580.811
——	hexyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₂H₄₁ClFN₅O₅	630.159
——	6-[(1-tert-butoxycarbonylpiperidin-4-yl)oxy]-4-(3-chloro-4-fluoroanilino)-7-methoxyquinazoline	609767-43-3	C₂₅H₂₈ClFN₄O₄	502.973
——	heptyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₃H₄₃ClFN₅O₅	644.186
——	dodecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₈H₅₃ClFN₅O₅	714.321
——	pentadecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₁H₅₉ClFN₅O₅	756.401
——	octyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₄H₄₅ClFN₅O₅	658.213
——	tetradecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₀H₅₇ClFN₅O₅	742.374
——	hexadecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₂H₆₁ClFN₅O₅	770.428
——	nonyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₅H₄₇ClFN₅O₅	672.24
——	decyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₆H₄₉ClFN₅O₅	686.267
——	icosyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₆H₆₉ClFN₅O₅	826.536
——	undecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₇H₅₁ClFN₅O₅	700.294
——	nonadecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₅H₆₇ClFN₅O₅	812.509
——	heptadecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₃H₆₃ClFN₅O₅	784.455
——	tridecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₃₉H₅₅ClFN₅O₅	728.348
——	octadecyl 4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)propyl)piperazin-1-yl)-4-oxobutanoate	——	C₄₄H₆₅ClFN₅O₅	798.482
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438072-53-7	C₂₄H₂₇ClFN₅O₂	471.962
——	N-(3-chloro-4-fluorophenyl)-6-(3-(hexahydro-1H-pyrrolo[3,4-b]pyridin-6(2H)-yl)propoxy)-7-methoxyquinazolin-4-amine	1438073-26-7	C₂₅H₂₉ClFN₅O₂	485.989

反应信息

作为反应物：

描述：

4-(3-氯-4-氟苯胺)-7-甲氧基-喹唑啉-6-醇在氨基磺酰氯作用下，反应 2.0h，以75%的产率得到4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl sulfamate

参考文献：

名称：

发现新型亮氨酰磺酸氨基磺酸替代物作为雷帕霉素复合物1（mTORC1）抑制剂的亮氨酰-tRNA合成酶（LRS）靶向的哺乳动物靶标

摘要：

根据最近的研究，亮氨酰-tRNA合成酶（LRS）充当亮氨酸传感器，并调节哺乳动物雷帕霉素复合物1（mTORC1）靶标的激活。由于过度活跃的mTORC1与包括结肠癌在内的多种疾病有关，因此靶向LRS的mTORC1抑制剂代表了抗癌治疗的潜在选择。在这项工作中，我们开发了一系列简化的亮氨苄基磺酸盐类似物，其中包含N-（3-氯-4-氟苯基）喹唑啉-4-胺部分来取代腺嘌呤基团。我们鉴定了几种与先前报道的抑制剂具有可比活性的化合物，并表现出选择性的mTORC1抑制和抗癌活性。这项研究进一步支持以下假设：LRS是调节mTORC1途径的有希望的靶标。

DOI：

10.1016/j.bmc.2018.06.034
作为产物：

描述：

藜芦酸在吡啶、盐酸、氯化亚砜、甲烷磺酸、 L-蛋氨酸、硫酸、氨、硝酸、铁粉、 N,N-二甲基甲酰胺作用下，以甲醇、乙醇、水、异丙醇为溶剂，反应 24.0h，生成 4-(3-氯-4-氟苯胺)-7-甲氧基-喹唑啉-6-醇

参考文献：

名称：

新型全氟化碳调节的4-苯胺基喹唑啉类似物的简便合成

摘要：

4-苯氨基喹唑啉类似物在许多抑制表皮生长因子受体（EGFR）酪氨酸激酶活性的小分子中脱颖而出，从而成为抗癌药物设计的重要分子靶标。本文中，通过各种苯胺喹唑啉与PFC衍生的甲磺酸盐的亲核取代反应，直接设计和制备了一系列新颖的全氟化碳（PFC）调节的4-苯胺基喹唑啉。在碱的存在下，反应平稳进行，从而以高收率或高收率得到了范围广泛的4-苯胺基喹唑啉，苯胺部分上具有不同的取代基。此外，吉非替尼和厄洛替尼的PFC修饰类似物也分别以93％和90％获得。19 F MRI。

DOI：

10.1002/cjoc.201700240

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文献信息

Ultrasmall dual-modality silica nanoparticle drug conjugates: Design, synthesis, and characterization

作者：Barney Yoo、Kai Ma、Li Zhang、Andrew Burns、Sonia Sequeira、Ingo Mellinghoff、Cameron Brennan、Ulrich Wiesner、Michelle S. Bradbury

DOI：10.1016/j.bmc.2015.09.050

日期：2015.11

conjugates (NDCs) which utilize protease sensitive linkers to attached drug compounds and imaging labels to a clinically translated class of ultrasmall silica nanoparticle (C′ dots). We describe the synthesis and characterization of these linker-drug constructs. Linkers incorporating dipeptide enzyme substrates are attached to analogs of a prototypical epidermal growth factor receptor tyrosine kinase

有效的癌症指导和基于颗粒的纳米治疗成像剂的物理化学设计和合成仍然是一项艰巨的任务。至关重要的是，对于旨在将其货物存放在疾病部位而无伴随剂量限制毒性的平台而言，展示其最大的输送，保留和治疗功效是至关重要的。在这项工作中，我们描述了双模态纳米颗粒药物共轭物（NDC），该共轭物利用蛋白酶敏感的接头将药物化合物和成像标记物标记为临床翻译的超小二氧化硅纳米颗粒（C'点）。我们描述了这些接头药物结构的合成和表征。结合了二肽酶底物的接头与原型表皮生长因子受体酪氨酸激酶抑制剂（EGFR-TKI）的类似物相连，对氨基苄氧羰基（PABC）。将这些构建体缀合到导致所需NDC的C'点上。这些NDC在模型蛋白酶的存在下显示出快速且可预测的释放动力学，并且在各种生物介质中稳定。最后，体外试验显示NDC在降低H1650细胞（一种人类肿瘤来源的细胞系）中的磷酸化EGFR水平方面具有很高的活性。数据表明，NDC表现出令
[EN] AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE<br/>[FR] DÉRIVÉS D'AMINOQUINAZOLINE ET LEURS SELS ET PROCÉDÉS D'UTILISATION

申请人：SUNSHINE LAKE PHARMA CO LTD

公开号：WO2013071697A1

公开（公告）日：2013-05-23

The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter-and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

本发明涉及医学领域。本文提供了氨基喹唑啉衍生物、其盐和药物配方，用于调节蛋白酪氨酸激酶活性，以及调节细胞间和/或细胞内信号传导。本文还提供了包含氨基喹唑啉化合物的药用可接受组合物，以及使用这些组合物治疗哺乳动物，特别是人类的增生性疾病的方法。
AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE

申请人：SUNSHINE LAKE PHARMA CO., LTD.

公开号：US20140228361A1

公开（公告）日：2014-08-14

The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

本发明涉及医学领域。本文提供了氨基喹唑啉衍生物，其盐和药物配方在调节蛋白酪氨酸激酶活性以及调节细胞间和/或细胞内信号传导方面具有用处。本文还提供了包含氨基喹唑啉化合物的药用可接受组合物，以及在治疗哺乳动物，特别是人类的增生性疾病中使用这些组合物的方法。
喹唑啉基羧酸酯类化合物及其用途

申请人：贾玉庆

公开号：CN107400094B

公开（公告）日：2020-04-03

本发明涉及一种含喹唑啉基的羧酸酯类化合物及其用途。所述的羧酸酯类化合物为式I所示化合物，或其在药学上可接受的盐。本发明提供的羧酸酯类化合物可用于制备广谱抗癌药物。式I中，R为由取代苯基或/和氨基取代的乙基，取代苯基，或取代吡啶基；所述取代苯基的取代基为或所述取代吡啶基的取代基为
Optimization of gefitinib analogues with potent anticancer activity

作者：Kai-Hao Yin、Yi-Han Hsieh、Rohidas S. Sulake、Su-Pei Wang、Jui-I. Chao、Chinpiao Chen

DOI：10.1016/j.bmcl.2014.09.056

日期：2014.11

The interactions of gefitinib (Iressa) in EGFR are hydrogen bonding and van der Waals forces through quinazoline and aniline rings. However the morpholino group of gefitinib is poorly ordered due to its weak electron density. A series of novel piperazino analogues of gefitinib where morpholino group substituted with various piperazino groups were designed and synthesized. Most of them indicated significant

EGFR中吉非替尼（Iressa）的相互作用是氢键和通过喹唑啉和苯胺环的范德华力。但是，由于吉非替尼的吗啉代基团电子强度较弱，因此排列较差。设计并合成了一系列新的吉非替尼哌嗪子基类似物，其中吗啉代基团被各种哌嗪子基团取代。他们中的大多数表明对人类癌细胞系具有显着的抗癌活性。特别是，化合物52 – 54对癌细胞具有极好的效力。已经开发了用于合成吉非替尼中间体的会聚合成方法，该中间体可导致吉非替尼以及许多类似物。