公开(公告)号：US20100190996A1

公开(公告)日：2010-07-29

申请号：US11990456

申请日：2005-12-21

申请人： Arava Veera Reddy ,  Siripalli Udaya Bhaskara Rao ,  Chinnapillai Rajendrian ,  Vankateswarlu Jasti

发明人： Arava Veera Reddy ,  Siripalli Udaya Bhaskara Rao ,  Chinnapillai Rajendrian ,  Vankateswarlu Jasti

IPC分类号： C07D403/10

CPC分类号： C07D403/10

摘要： The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.

摘要翻译： 本发明涉及一种制备氯沙坦的改进方法。 该方法包括在相转移催化剂和碱的存在下使2-正丁基-4-氯-5-甲酰基咪唑与2-（4-溴甲基）苄腈反应，并还原所得的氰醛以产生氰基醇 其进一步与叠氮化钠在N-甲基吡咯烷酮和盐中反应以制备氯沙坦。

公开(公告)号：US07385072B2

公开(公告)日：2008-06-10

申请号：US11478552

申请日：2006-06-29

申请人： Jasti Venkateswarlu ,  Arava Veera Reddy ,  Chinnapillai Rajendiran ,  Samjuddin Md Md

发明人： Jasti Venkateswarlu ,  Arava Veera Reddy ,  Chinnapillai Rajendiran ,  Samjuddin Md Md

IPC分类号： C07C255/08

CPC分类号： C07C253/30 ,  C07C255/41

摘要： The invention disclosed in this application relates to an improved process for the preparation of Entacapone. In one embodiment the process involves: (i) reacting a 3-alkoxy-4-hydroxy-5-nitrobenzadehyde with N,N-diethylaminocyanoacetamide in the presence of a mild acid catalyst and a solvent, to provide a 3-O-alkylated Entacapone, and treating the 3-O-alkylated Entacapone with an acid catalyst in the presence of an organic base to provide Entacapone.

摘要翻译： 本申请中公开的发明涉及一种改进的恩他卡朋制备方法。 在一个实施方案中，该方法包括：（i）在温和的酸催化剂和溶剂的存在下使3-烷氧基-4-羟基-5-硝基苯甲酸与N，N-二乙基氨基氰基乙酰胺反应，得到3-O-烷基化的恩他卡朋 ，并在有机碱存在下用酸催化剂处理3-O-烷基化的恩他卡朋，以提供恩他卡朋。

公开(公告)号：US07923566B2

公开(公告)日：2011-04-12

申请号：US11990456

申请日：2005-12-21

申请人： Arava Veera Reddy ,  Siripalli Udaya Bhaskara Rao ,  Chinnapillai Rajendiran ,  Venkateswarlu Jasti

发明人： Arava Veera Reddy ,  Siripalli Udaya Bhaskara Rao ,  Chinnapillai Rajendiran ,  Venkateswarlu Jasti

IPC分类号： C07D403/10 ,  C07D257/00 ,  C07F5/06

CPC分类号： C07D403/10

摘要： The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.

摘要翻译： 本发明涉及一种制备氯沙坦的改进方法。 该方法包括在相转移催化剂和碱的存在下使2-正丁基-4-氯-5-甲酰基咪唑与2-（4-溴甲基）苄腈反应，并还原所得的氰醛以产生氰基醇 其进一步与叠氮化钠在N-甲基吡咯烷酮和盐中反应以制备氯沙坦。

公开(公告)号：US07915425B2

公开(公告)日：2011-03-29

申请号：US11991123

申请日：2005-12-21

申请人： Arava Veera Reddy ,  Siripalli Udaya Bhaskara Rao ,  Chinnapillai Rajendiran ,  Venkateswarlu Jasti

发明人： Arava Veera Reddy ,  Siripalli Udaya Bhaskara Rao ,  Chinnapillai Rajendiran ,  Venkateswarlu Jasti

IPC分类号： C07D257/04 ,  C07D233/68

CPC分类号： C07D403/10

摘要： The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method.

摘要翻译： 本发明涉及一种制备氯沙坦及其钾盐的改进方法，其包括：（i）在碱和相转移催化剂的存在下使溴OTBN与BCFI反应产生氰醛; 在三丁基氯化锡存在下，使形成的氰基醛与叠氮化钠反应生成醛四唑; 用硼氢化钠还原形成的醛四唑以产生氯沙坦; 如果需要，通过已知的方法将形成的氯沙坦转化成其钾盐。

公开(公告)号：US20100222597A1

公开(公告)日：2010-09-02

申请号：US11991123

申请日：2005-12-21

申请人： Arava Veera Reddy

发明人： Arava Veera Reddy

IPC分类号： C07D403/10

CPC分类号： C07D403/10

摘要： The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method.

摘要翻译： 本发明涉及一种制备氯沙坦及其钾盐的改进方法，其包括：（i）在碱和相转移催化剂的存在下使溴OTBN与BCFI反应产生氰醛; 在三丁基氯化锡存在下，使形成的氰基醛与叠氮化钠反应生成醛四唑; 用硼氢化钠还原形成的醛四唑以产生氯沙坦; 如果需要，通过已知的方法将形成的氯沙坦转化成其钾盐。