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N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑 | 124750-51-2

物质功能分类

原料药 - 循环系统用药 - 抗高血压病药

分子结构分类

有机化合物 - 苯类化合物 - 三苯基化合物

中文名称

N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑

中文别名

5-(4-溴甲基-1,1-联苯-2-基)-1-三苯甲基四唑；N-三苯基甲基5-(4-溴甲基二苯基-2-基)四唑E；5-[4'-溴甲基联苯-2-基]-1-三苯甲基-1H-四氮唑；5-(4'-溴甲基联苯-2-基)-1-三苯基甲基四氮唑；溴代坎地沙坦杂质；奥美沙坦杂质；TTBB；奥美沙坦中间体；BBTT；N-(三苯基甲基)-5-(4)-溴甲基联苯-2-基)四氮唑；N-(三苯基甲基)-5-(4-溴甲基联苯-2-基)四氮唑

英文名称

N-(triphenylmethyl)-5-(4'-bromomethylbiphenyl-2-yl)tetrazole

英文别名

5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole；4-[2-(trityltetrazol-5-yl)phenyl]benzyl bromide；5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-triphenylmethyl-1H-tetrazole；5-(4'-(bromomethyl)biphenyl-2-yl)-1-trityl-1H-tetrazole；5-(4'-Bromomethyl-1,1'-biphenyl-2-yl)-1-triphenylmethyl-1H-tetrazole；5-[2-[4-(bromomethyl)phenyl]phenyl]-1-trityltetrazole

CAS

124750-51-2

化学式

C₃₃H₂₅BrN₄

mdl

——

分子量

557.492

InChiKey

ZTFVTXDWDFIQEU-UHFFFAOYSA-N

BEILSTEIN

——

EINECS

——

物化性质

熔点：

152-155°C
沸点：

61°C/12mmHg(lit.)
密度：

1.28±0.1 g/cm3(Predicted)
溶解度：

Soluble in Chloroform and Methanol (Sparingly)
稳定性/保质期：

| Moisture Sensitive |

计算性质

辛醇/水分配系数(LogP)：

8.2
重原子数：

38
可旋转键数：

7
环数：

6.0
sp3杂化的碳原子比例：

0.06
拓扑面积：

43.6
氢给体数：

0
氢受体数：

3

安全信息

危险等级：

6.1
储存条件：

-20°C 冰箱

SDS

SDS：eeb163905daba6169f5e6dd56d1edba8

查看

制备方法与用途

用途：用于制备药物依贝沙坦的中间体。

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
N-(三苯基甲基)-5-(4’-甲基联苯-2-基)四氮唑	N-triphenylmethyl-5-(4'-methylbiphenyl-2-yl)tetrazole	124750-53-4	C₃₃H₂₆N₄	478.596
奥美沙坦杂质81	5-<2-(4'-formylbiphenylyl)>-2-(triphenylmethyl)-2H-tetrazole	155983-56-5	C₃₃H₂₄N₄O	492.58
5-[4’-羟基甲基-(1,1’-联苯)-2-基]-2-三苯基甲基四唑	4'-hydroxymethyl-2-(N-trityl-1H-tetrazol-5-yl)biphenyl	154709-18-9	C₃₃H₂₆N₄O	494.596
——	5-<4'-Methyl-1,1'-biphenyl-2-yl>-1H-tetrazole-1-propanenitrile	120568-17-4	C₁₇H₁₅N₅	289.34

下游产品

中文名称	英文名称	CAS号	化学式	分子量
奥美沙坦杂质81	5-<2-(4'-formylbiphenylyl)>-2-(triphenylmethyl)-2H-tetrazole	155983-56-5	C₃₃H₂₄N₄O	492.58
5-[4’-羟基甲基-(1,1’-联苯)-2-基]-2-三苯基甲基四唑	4'-hydroxymethyl-2-(N-trityl-1H-tetrazol-5-yl)biphenyl	154709-18-9	C₃₃H₂₆N₄O	494.596
——	1-(2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)methanamine	134603-82-0	C₃₃H₂₇N₅	493.611
——	[2'-(N-Triphenylmethyl-tetrazol-5-yl)-biphenyl-4-yl]methyl azide	124806-66-2	C₃₃H₂₅N₇	519.608
——	N-pentyl-N-[[2'-[N-(triphenylmethyl)tetrazol-5-yl]-1,1'-biphenyl-4-yl]methyl]amine	141872-29-9	C₃₈H₃₇N₅	563.745
——	(S)-2-[2'-(1-Trityl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]aminopropan-1-ol	1043608-26-9	C₃₆H₃₃N₅O	551.691
——	N-((2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-4H-1,2,4-triazol-4-amine	——	C₃₅H₂₈N₈	560.661
——	(2-[2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]aminoethyl)carbamic acid t-butyl ester	1043607-83-5	C₄₀H₄₀N₆O₂	636.797
——	2-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methylsulfanyl]-1H-benzimidazole	1247013-51-9	C₄₀H₃₀N₆S	626.784
——	methyl α-(1-oxopentyl)-2'-<1-(triphenylmethyl)-1H-tetrazol-5-yl><1,1'-biphenyl>-4-propanoate	144757-33-5	C₄₁H₃₈N₄O₃	634.778
——	5-ethyl-2-imino-3-[2'-(1-triphenyl-methyl-1H-tetrazol-5-yl)biphenyl-4-yl]methyl-1,3,4-thiadiazoline	178859-91-1	C₃₇H₃₁N₇S	605.766
——	2-butyl-1-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-1H-imidazole-4-carbaldehyde	1206696-90-3	C₄₁H₃₆N₆O	628.776
三苯甲基缬沙坦	N-pentanoyl-N-(4-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)phenyl)methyl-L-valine	783369-52-8	C₄₃H₄₃N₅O₃	677.846
——	2-butyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carbaldehyde	905456-95-3	C₄₁H₃₆N₆O	628.776
——	6-butyl-2-methyl-5-<<2'-<1-(triphenylmethyl)-1H-tetrazol-5-yl><1,1'-biphenyl>-4-yl>methyl>pyrimidin-4(1H)-one	148564-13-0	C₄₂H₃₈N₆O	642.803
——	(1S)-N-(1-hydroxymethyl-2-methyl-propyl)-N'-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-thiophene-2-carboxamide	1033772-55-2	C₄₃H₃₉N₅O₂S	689.881
(S)-3-甲基-2-(n-((2-(1-三苯甲游基-1H-四唑-5-基)-[1,1-联苯]-4-基)甲基)戊酰胺)丁酸甲酯	methyl 3-methyl-2-[pentanoyl-[[4-[2-(1-trityltetrazole-5-yl)phenyl]phenyl]methyl]amino]butyrate	781664-81-1	C₄₄H₄₅N₅O₃	691.873
——	5-propyl-1-[2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-pyrazole-3-carboxylic acid ethyl ester	1260231-30-8	C₄₂H₃₈N₆O₂	658.803
——	2-n-Butyl-4,5-dicyano-1-[(2'-(N-triphenylmethyl(1H-tetrazol-5-yl))-biphenyl-4-yl)methyl]imidazole	124779-27-7	C₄₂H₃₄N₈	650.786
——	3-benzyl-6-chloro-1-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidine-2,4(1H,3H)-dione	137016-24-1	C₄₄H₃₃ClN₆O₂	713.238
——	2-benzyl-3-[[2'-[1-(triphenylmethyl)-1H-tetrazol-5-yl]-(1,1'-biphenyl)-4-yl]methyl]-2,3-diazaspiro[4.4]nonane-1,4-dione	291774-03-3	C₄₇H₄₀N₆O₂	720.874
——	5-propyl-2-[2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2H-pyrazole-3-carboxylic acid ethyl ester	1260231-31-9	C₄₂H₃₈N₆O₂	658.803
——	N-[(2'-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-N-valeroyl-(L)-valine benzyl ester	137864-44-9	C₅₀H₄₉N₅O₃	767.971
——	6-chloro-3-ethyl-1-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidine-2,4(1H,3H)-dione	——	C₃₉H₃₁ClN₆O₂	651.167
——	8-butyl-7-[[2'-[1-(triphenylmethyl)-1H-tetrazol-5-yl]-(1,1'-biphenyl)-4-yl]methyl]-7,8-diazaspiro[4.5]decane-6,9-dione	——	C₄₅H₄₄N₆O₂	700.883
——	2-ethyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1027922-63-9	C₃₉H₃₂N₈	612.737
——	3-Butyl-2-{[2'-(N-triphenylmethyl-tetrazol-5-yl)-biphenyl-4-yl]methyl}-isoquinolin-1(2H)-one	——	C₄₆H₃₉N₅O	677.849
2-丁基-4-氯-1-{[2'-(1-三苯甲基-1H-四唑-5-基)-4-联苯基]甲基}-1H-咪唑-5-甲醛	2-butyl-5-chloro-3-[2’-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3Himidazole-4-carbaldehyde	120568-18-5	C₄₁H₃₅ClN₆O	663.221
[2-丁基-4-氯-1-[(2’-(1-三苯甲基-1H-四氮唑-5-基)联苯-4-基)甲基)-1H-咪唑-5-基)甲醇	N-trityllosartan	124751-00-4	C₄₁H₃₇ClN₆O	665.237
——	3-butyl-6-chloro-1-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidine-2,4(1H,3H)-dione	——	C₄₁H₃₅ClN₆O₂	679.221
——	2,7-dimethyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026875-46-6	C₃₉H₃₂N₈	612.737
——	2,6-dimethyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026628-06-7	C₃₉H₃₂N₈	612.737
——	5-(4-methoxycarbonylbenzyl)-6-methyl-2-propyl-4-[2'-(triphenylmethyltetrazol-5-yl)biphenyl-4-yl]methoxypyrimidine	161946-64-1	C₅₀H₄₄N₆O₃	776.938
——	(4S)-3-[2'-(1-triphenylmethyl-1H-tetrazole-5-yl)-biphenyl-4-yl-methyl]-4-isopropyl-2-(2-thienyl)-1,3-oxazolidine	1033772-57-4	C₄₃H₃₉N₅OS	673.882
——	2-n-Butyl-6-methoxycarbonylmethyl-3-[[2'-(N-triphenylmethyltetrazol-5-yl)biphenyl-4-yl]methyl]-4(3H)-pyrimidone	137443-24-4	C₄₄H₄₀N₆O₃	700.84
——	2,6-diethyl-1-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-pyrazolo[1,5-b][1,2,4]triazole	203176-85-6	C₄₁H₃₆N₈	640.79
——	6-methyl-2-propyl-1-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-pyrazolo[1,5-b][1,2,4]triazole	1027930-42-2	C₄₁H₃₆N₈	640.79
三苯甲基厄贝沙坦	trityl irbesartan	138402-10-5	C₄₄H₄₂N₆O	670.857
——	2-ethyl-7-methyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026907-56-1	C₄₀H₃₄N₈	626.764
——	2-ethyl-6-methyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026614-20-9	C₄₀H₃₄N₈	626.764
——	7-Ethyl-2-methyl-5-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026128-50-6	C₄₀H₃₄N₈	626.764
——	6-ethyl-2-methyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1027661-83-1	C₄₀H₃₄N₈	626.764
——	7-methyl-2-propyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026255-46-8	C₄₁H₃₆N₈	640.79
——	2-Methyl-7-propyl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-b][1,2,4]triazole	1027507-49-8	C₄₁H₃₆N₈	640.79
——	6-methyl-2-propyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl-]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1027179-12-9	C₄₁H₃₆N₈	640.79
——	2-methyl-6-propyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026492-50-1	C₄₁H₃₆N₈	640.79
——	2-Propyl-1-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]methyl]-1H-imidazo[1,2-c]imidazole-7-carbonitrile	149323-16-0	C₄₂H₃₄N₈	650.786
——	2-Butyl-6-ethenyl-3-[[2'-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1'-biphenyl]-4-yl]methyl]-4(3H)-quinazolinone	154475-78-2	C₄₇H₄₀N₆O	704.874
——	3-Benzyl-6-butyl-2-methyl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-4-one	172292-50-1	C₄₉H₄₄N₆O	732.928
——	2,6-diethyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	203176-87-8	C₄₁H₃₆N₈	640.79
——	2-ethyl-5-(2'-ethoxycarbonylethyl)-6-methyl-3-[[2'-(N-triphenyl-methyltetraazol-5-yl)biphenyl-4-yl]methyl]-pyrimidine-4(3H)-one	178554-88-6	C₄₅H₄₂N₆O₃	714.867
——	4-isobutyryl-2-propyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carbonitrile	144691-06-5	C₄₄H₃₉N₇O	681.84
——	2,7-diethyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1027550-22-6	C₄₁H₃₆N₈	640.79
——	2-propyl-4-pivaloyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carbonitrile	144691-00-9	C₄₅H₄₁N₇O	695.867
——	2-butyl-4-isobutyryl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carbonitrile	144691-09-8	C₄₅H₄₁N₇O	695.867
——	2-Butyl-6-(1-hydroxyethyl)-3-[[2'-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1'-biphenyl]-4-yl]methyl]-4(3H)-quinazolinone	——	C₄₇H₄₂N₆O₂	722.889
——	2-Ethyl-7-propan-2-yl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-b][1,2,4]triazole	1027442-84-7	C₄₂H₃₈N₈	654.817
——	7-ethyl-2-isopropyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026463-33-1	C₄₂H₃₈N₈	654.817
——	2-ethyl-6-propyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026458-04-7	C₄₂H₃₈N₈	654.817
——	6-ethyl-2-propyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1028264-08-5	C₄₂H₃₈N₈	654.817
——	2-butyl-4-pivaloyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carbonitrile	144691-03-2	C₄₆H₄₃N₇O	709.894
——	2-propyl-1-[2'-(1-triphenylmethyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-imidazole-4,5-dicarboxylic acid dimethyl ester	124750-61-4	C₄₃H₃₈N₆O₄	702.813
——	2-Ethyl-7-propyl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-b][1,2,4]triazole	1026478-77-2	C₄₂H₃₈N₈	654.817
——	6-butyl-2-ethyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1026891-21-3	C₄₃H₄₀N₈	668.844
——	7-ethyl-2-propyl-5-[[2'-(N-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl]methyl]-5H-pyrazolo[1,5-b][1,2,4]triazole	1027201-38-2	C₄₂H₃₈N₈	654.817
——	Ethyl 2-propyl-1-[[2'-(N-triphenylmethyltetrazol-5-yl)biphenyl-4-yl]methyl]indole-7-carboxylate	149323-30-8	C₄₇H₄₁N₅O₂	707.875
三苯甲基奥美沙坦酸	4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl) methyl)-1H-imidazole-5-carboxylic acid	761404-85-7	C₄₃H₄₀N₆O₃	688.829
非马沙坦杂质1	2-n-butyl-5-(N,N-dimethylaminothioformylmethyl)-6-methyl-3-[[2'-(N-triphenylmethyl-5-tetrazolyl)biphenyl]-4-methyl]pyrimidin-4-one	1361024-52-3	C₄₆H₄₅N₇OS	743.976
——	5-cyano-4-(1-hydroxy-1-methylpropyl)-2-propyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole	144690-39-1	C₄₄H₄₁N₇O	683.856
——	7-Butyl-2-ethyl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-b][1,2,4]triazole	1026324-06-0	C₄₃H₄₀N₈	668.844
——	dimethyl 2-butyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-4,5-dicarboxylate	140199-57-1	C₄₄H₄₀N₆O₄	716.839
三苯甲基坎地沙坦甲酯	methyl 2-ethoxy-1-<<2'-biphenyl-4-yl>methyl>-1H-benzimidazole-4-carboxylate	150058-29-0	C₄₄H₃₆N₆O₃	696.808
——	2-butyl-5-cyano-4-(1-hydroxy-1-methylpropyl)-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole	144690-37-9	C₄₅H₄₃N₇O	697.883
——	4-(naphth-1-yl)-2-n-propyl-1-[(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl)) biphenyl-4-yl)methyl]imidazole-5-carboxaldehyde	169504-87-4	C₅₀H₄₀N₆O	740.907
——	2-[4-(Benzyloxy)phenyl]-5-n-butyl-2,4-dihydro-4-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]-methyl]-3H-1,2,4-triazol-3-one	——	C₅₂H₄₅N₇O₂	799.975
奥美沙坦酯杂质R	2-propyl-1-[2'-(1-triphenylmethyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-imidazole-4,5-dicarboxylic acid diethyl ester	144690-53-9	C₄₅H₄₂N₆O₄	730.866
——	2-(1-hydroxybutyl)-3-((2’-(1-trityl-1H-tetrazol-5-yl)-[1,1’-biphenyl]-4-yl)methyl)-1,3-diazaspiro[4.4]non-1-en-4-one	——	C₄₄H₄₂N₆O₂	686.856
N-三苯甲基坎地沙坦甲基酯-d4	methyl 2-ethoxy-1-<<2'-biphenyl-4-yl>methyl>-1H-benzimidazole-7-carboxylate	150058-32-5	C₄₄H₃₆N₆O₃	696.808
——	methyl 4-(1-hydroxy-1-methylethyl)-2-methoxymethyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	153282-91-8	C₄₃H₄₀N₆O₄	704.828
——	4-(1-hydroxyethyl)-1-[2'-(1-triphenylmethyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2-propyl-1H-imidazole-5-carboxylic acid ethyl ester	144690-58-4	C₄₄H₄₂N₆O₃	702.856
——	6-Butyl-2-methyl-3-(thiophen-2-ylmethyl)-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-4-one	172292-51-2	C₄₇H₄₂N₆OS	738.956
——	ethyl 2-ethyl-4-(1-hydroxy-1-methylethyl)-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	144690-95-9	C₄₄H₄₂N₆O₃	702.856
——	2-Butyl-6-(2-furanylhydroxymethyl)-3-[2'-[1-(triphenylmethyl)-1H-tetrazol-5-yl][1,1'biphenyl]-4-yl]methyl-4(3H)-quinazolinone	155399-66-9	C₅₀H₄₂N₆O₃	774.922
——	ethyl 2-ethoxymethyl-4-(1-hydroxy-1-methylethyl)-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	153282-99-6	C₄₅H₄₄N₆O₄	732.882
——	propyl 4-(1-hydroxy-1-methylethyl)-2-propoxymethyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	153283-08-0	C₄₇H₄₈N₆O₄	760.936
三苯甲基奥美沙坦乙酯	ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylate	144690-33-5	C₄₅H₄₄N₆O₃	716.883
——	2,7-Diethyl-6-methyl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-b][1,2,4]triazole	1026132-84-2	C₄₂H₃₈N₈	654.817
——	4-(2,5-dimethyl-1H-pyrrol-1-yl)-2-propyl-1-[[2'-(N-triphenylmethyl-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl]-1H-imidazole-5-carboxaldehyde	150537-90-9	C₄₆H₄₁N₇O	707.878
——	ethyl 2-butyl-4-(1-hydroxy-1-methylethyl)-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	144690-36-8	C₄₆H₄₆N₆O₃	730.91
——	6-chloro-5-phenyl-3-propyl-1-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidine-2,4(1H,3H)-dione	137016-25-2	C₄₆H₃₇ClN₆O₂	741.292
——	methyl 2-<<4-butyl-2-methyl-6-oxo-5-<<2'-<1-(triphenylmethyl)-1H-tetrazol-5-yl><1,1'-biphenyl>-4-yl>methyl>-1(6H)-pyrimidinyl>methyl>benzoate	148597-80-2	C₅₁H₄₆N₆O₃	790.965
——	ethyl 4-(1-hydroxy-1-methylethyl)-2-methylthio-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	——	C₄₃H₄₀N₆O₃S	720.895
——	1-[(2'-(1-triphenylmethyltetrazol-5-yl)biphenyl-4-yl)methyl]-2-n-butyl-5,6-dimethyl-1H-benzimidazol-4,7-dione	145982-30-5	C₄₆H₄₀N₆O₂	708.863
——	ethyl 2-((tert-butoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate	906474-56-4	C₄₇H₄₂N₆O₆	786.887
——	2-phenyl-3-[[2'-[1-(triphenylmethyl)-1H-tetrazol-5-yl]-(1,1'-biphenyl)-4-yl]methyl]-2,3-diazaspiro[4.4]nonane-1,4-dione	291774-01-1	C₄₆H₃₈N₆O₂	706.847
——	2-butyl-4-chloro-1,6-dihydro-6-methyl-1-<<2'-<1-(triphenylmethyl)tetrazole-5-yl><1,1'-biphenyl>-4-yl>methyl>pyrimidine-5-carboxylic acid, diphenylmethyl ester	145319-03-5	C₅₆H₄₉ClN₆O₂	873.497
——	2,6,7-Triethyl-5-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-b][1,2,4]triazole	1028279-69-7	C₄₃H₄₀N₈	668.844
——	Methyl 2,8-diethoxy-7-[[2'-(N-trityltetrazol-5-yl)biphenyl-4-yl]methyl]purine-6-carboxylate	149323-22-8	C₄₄H₃₈N₈O₄	742.837
——	pivaloyloxymethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-{4-[2-(trityltetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate	144690-34-6	C₄₉H₅₀N₆O₅	802.973

反应信息

作为反应物：

描述：

N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑在硫酸、水、 potassium carbonate 、 potassium hydroxide 、 lithium hydroxide 作用下，以水、 N,N-二甲基甲酰胺、丙酮、乙腈为溶剂，反应 9.5h，生成奥美沙坦酯

参考文献：

名称：

一种奥美沙坦酯的制备方法

摘要：

本发明提供了一种制备奥美沙坦酯的改进方法，属于医药合成领域。该方法包括以下步骤：以咪唑单酯和四溴联苯四氮唑(BBTT)为起始原料，在丙酮体系中“一锅法”经缩合、水解、酸化得到4-(1-羟基-1-甲基乙基)-2-丙基-1-{4-[2-(三苯甲基四唑-5-基)苯基]苯基}甲基咪唑-5-羧酸，后与4-氯甲基-5-甲基-1，3-二氧杂环戊烯-2-酮酯化，酯化物经纯化纯度≥99.5％，后在22.5％硫酸溶液作用下脱保护得到高纯度的奥美沙坦酯。本发明缩合和酯化采用一锅法简化了操作流程，易于控制，且反应中对关键中间体酯化物进行纯化后脱保护可得到纯度≥99.5％奥美沙坦酯，总产率可达60-75％，原料易得，成本低，适合于工业化生产。

公开号：

CN105481842A
作为产物：

描述：

4,4-dimethyl-2-(4'-methylbiphenyl-2-yl)oxazoline 在盐酸、 N-溴代丁二酰亚胺(NBS) 、氯化亚砜、叠氮基三甲基硅烷、 N,N-二异丙基乙胺、三苯基膦、 sodium hydroxide 、偶氮二甲酸二乙酯作用下，以四氢呋喃、甲醇、四氯化碳、水为溶剂，生成 N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑

参考文献：

名称：

1,(3,)5-substituted imidazoles, useful in the treatment of hypertension and methods for their preparation

摘要：

公开号：

EP2162441B1
作为试剂：

描述：

2-丁基-1,6-二氢-N,N,4-三甲基-6-氧代-5-嘧啶乙酰胺、 N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑在 N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑作用下，生成 2-丁基-1,6-二氢-N,N,4-三甲基-6-氧代-1-[[2'-[1-(三苯甲基)-1H-四氮唑-5-基][1,1'-联苯]-4-基]甲基]-5-嘧啶乙酰胺

参考文献：

名称：

[EN] NOVEL PREPARATION METHOD OF 2-(2-N-BUTYL-4-HYDROXY-6-METHYL-PYRIMIDIN-5-YL)-N,N-DIMETHYLACETAMIDE
[FR] NOUVEAU PROCÉDÉ DE PRÉPARATION DE 2-(2-N-BUTYL-4-HYDROXY-6-MÉTHYL-PYRIMIDIN-5-YL)-N,N-DIMÉTHYLACÉTAMIDE

摘要：

本发明提供了一种制备2-(2-n-丁基-4-羟基-6-甲基嘧啶-5-基)-N,N-二甲基乙酰胺的方法，包括在碱的存在下将以下式2的化合物与戊胺基或其盐反应。[式2]其中R1代表C1-C6线性或支链烷基或C3-C6环烷基。此外，本发明还提供了一种制备2-(2-n-丁基-4-羟基-6-甲基嘧啶-5-基)-N,N-二甲基乙酰胺的方法，包括以下步骤：a) 在碱的存在下，将2-(2-n-丁基-4-羟基-6-甲基嘧啶-5-基)-乙酸与卤代甲酸酯化合物反应，b) 将步骤a)的产物与二甲胺反应。

公开号：

WO2011090323A2

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文献信息

Improved Sommelet Reaction Catalysed by Lanthanum Triflate

作者：Wenhao Xu、Weike Su

DOI：10.3184/174751914x14175125259964

日期：2014.12

An improved Sommelet reaction for the synthesis of araldehydes from benzyl halides and hexamethylenetetramine was achieved employing lanthanum triflate (3 mol%) as catalyst in water with sodium dodecyl sulfate (SDS, 2 wt%) as solubiliser. Good to excellent yields were obtained in most of the 18 examples.

使用三氟甲磺酸镧 (3 mol%) 作为催化剂，在水中使用十二烷基硫酸钠 (SDS, 2 wt%) 作为增溶剂，实现了用于从苄基卤化物和六亚甲基四胺合成芳醛的改进 Sommelet 反应。在 18 个实施例中的大多数中获得了良好到极好的产率。
Angiotensin II receptor blocking 2,3,6 substituted quinazolinones

申请人：American Cyanamid Company

公开号：US05294611A1

公开（公告）日：1994-03-15

The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.

这项发明提供了具有以下结构式的新型2,3,6取代喹唑啉酮：##STR1## 其中R.sup.6、R和X如规范中所述，具有作为血管紧张素II（AII）拮抗剂的活性。
A process for the preparation or purification of olmesartan medoxomil

申请人：LEK Pharmaceuticals d.d.

公开号：EP2022790A1

公开（公告）日：2009-02-11

The present invention relates to a process for the preparation and purification of olmesartan medoxomil. The invention also relates to products obtainable by the process of the invention, to pharmaceutical compositions comprising the products and to their use in medicine, particularly to treat hypertension.

本发明涉及一种用于制备和纯化奥美沙坦酯酯的方法。该发明还涉及通过该方法获得的产品，包括含有这些产品的药物组合物以及它们在医学上的应用，特别是用于治疗高血压。
Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their

申请人：Sankyo Company, Limited

公开号：US05616599A1

公开（公告）日：1997-04-01

Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.sub.p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.

以下式(I)或式(I).sub.p的化合物：其中R.sup.1是烷基或烯基；R.sup.2和R.sup.3是氢、烷基、烯基、环烷基、芳基烷基、芳基或与环烷基融合的芳基；R.sup.4是氢、烷基、烷酰基、烯酰基、芳基羰基、烷氧羰基、四氢吡喃基、四氢硫代吡喃基、四氢噻吩基、四氢呋喃基，具有式--SiR.sup.a R.sup.b R.sup.c的基团，其中R.sup.a、R.sup.b和R.sup.c是烷基或芳基、烷氧甲基、(烷氧基烷氧基)甲基、卤代烷氧甲基、芳基烷基、芳基或烷酰氧甲氧羰基；R.sup.5是羧基或--CONR.sup.8 R.sup.9，其中R.sup.8和R.sup.9是氢或烷基，或R.sup.8和R.sup.9一起形成亚烷基；R.sup.6是氢、烷基、烷氧基或卤素；R.sup.7是羧基或四唑-5-基；R.sub.p.sup.1是氢、烷基、环烷基或烷酰基；R.sub.p.sup.2是单键、烷基或烷基亚甲基；R.sub.p.sup.3和R.sub.p.sup.4分别是氢或烷基；R.sub.p.sup.6是羧基或四唑-5-基；X.sub.p是氧或硫；以及其药学上可接受的盐和酯。这些化合物是AII受体拮抗剂，因此具有降压活性，可用于治疗和预防高血压。这些化合物可以通过将联苯甲基化合物与咪唑化合物反应制备而成。
[EN] PROCESS FOR OLMESARTAN MEDOXOMIL<br/>[FR] PROCÉDÉ DE PRÉPARATION D'OLMÉSARTAN MÉDOXOMIL

申请人：HETERO RESEARCH FOUNDATION

公开号：WO2012001694A1

公开（公告）日：2012-01-05

The present invention provides a process for the preparation of substantially pure trityl olmesartan medoxomil. The present invention also provides a process for purification of trityl olmesartan medoxomil. The present invention further provides a process for purification of olmesartan medoxomil.

本发明提供了一种用于制备基本纯的三苯甲基奥美沙坦酯的方法。本发明还提供了一种用于纯化三苯甲基奥美沙坦酯的方法。本发明还提供了一种用于纯化奥美沙坦酯的方法。