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公开(公告)号：KR101251741B1
公开(公告)日：2013-04-05
申请号：KR1020100129430
申请日：2010-12-16
Applicant: 동화약품주식회사
IPC: C07D403/10 , A61K31/4184 , A61K31/4178 , A61P9/12
CPC classification number: Y02P20/55
Abstract: 본 발명은 칸데사르탄실렉세틸의 개선된 제조방법에 관한 것으로서, 트리틸칸데사르탄실렉세틸 화합물인 (± )-1-(사이클로헥실옥시카르보닐옥시)에틸-2-에톡시-1-[[2′-(N-트리페닐메틸-1H-테트라졸-5-일)바이페닐-4-일]메틸-1H-벤즈이미다졸-7-카르복실레이트의 트리페닐메탄 보호기를 제거하는 방법으로 알코올에 아세틸클로라이드를 첨가한 용액을 사용하여 트리페닐메탄 보호기를 제거함으로써 칸데사르탄실렉세틸을 제조하는 것이다.
본 발명에 따른 칸데사르탄실렉세틸의 제조방법은 유기용매에서 긴 시간 동안 환류교반이 필요치 않고, 염화수소 가스를 사용하지 않아 위험하지 않고, 전체적인 반응공정이 온화한 조건에서 단순화되어 대량생산에 적합하다. 특히 제조수율도 크게 향상되면서 아주 높은 순도의 칸데사르탄실렉세틸을 제조하는 방법을 제공한다.-
公开(公告)号：KR1020110094751A
公开(公告)日：2011-08-24
申请号：KR1020100014346
申请日：2010-02-17
Applicant: 동화약품주식회사
IPC: C07D403/10 , C07D403/04 , C07D403/06
CPC classification number: C07D403/04
Abstract: PURPOSE: A method for preparing telmisartan is provided to easily remove inorganic salt using a reaction solvent and to simplify reaction process without a separate process. CONSTITUTION: A method for preparing telmisartan of chemical formula 1 comprises: a step of condensing a compound of chemical formula 2 and a compound of chemical formula 3 using dimethyl sulfoxide and isopropanol to prepare a compound of chemical formula 4; and a step of hydrolyzing the compound of chemical formula 4 in a mixture solvent of methanol and purified water.
Abstract translation: 目的：提供替米沙坦制备方法，以便使用反应溶剂轻松除去无机盐，并简化反应过程，无需单独的工艺。 构成：化学式1的替米沙坦的制备方法包括：使用二甲基亚砜和异丙醇将化学式2的化合物与化学式3的化合物缩合以制备化学式4的化合物的步骤; 以及在甲醇和净化水的混合溶剂中水解化学式4的化合物的步骤。
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3.发明公开
公开(公告)号：KR1020110054670A
公开(公告)日：2011-05-25
申请号：KR1020090111413
申请日：2009-11-18
Applicant: 동화약품주식회사
IPC: C07C253/00 , C07C255/40 , A61K31/277
Abstract: PURPOSE: A process for preparing 2-cyano-3-hydroxy-N-[(4-trifluoromethyl)phenyl]but-2-enamide is provided to easily remove by-products generated during the manufacturing process of final products. CONSTITUTION: A process for preparing 2-cyano-3-hydroxy-N-[(4-trifluoromethyl)phenyl]but-2-enamide of chemical formula 1 from a compound of chemical formula 5 comprises the steps of: activating a compound of chemical formula 2 to an esterified compound using a carbodiimide compound; and reacting the resultant with a compound of chemical formula 4 to prepare a compound of chemical formula 5. The carbodiimide compound is selected from 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride, 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide, 1,3-diisopropylcarbodiimide or 1,3-dicyclohexylcarbodiimide.
Abstract translation: 目的：提供2-氰基-3-羟基-N - [（4-三氟甲基）苯基]丁-2-烯酰胺的制备方法，以便容易地除去最终产品的制造过程中产生的副产物。 构成：由化学式5的化合物制备化学式1的2-氰基-3-羟基-N - [（4-三氟甲基）苯基]丁-2-烯酰胺的方法包括以下步骤：活化化学式 式2与使用碳二亚胺化合物的酯化化合物反应; 将所得物与化学式4的化合物反应，制备化学式5的化合物。碳二亚胺化合物选自1- [3-（二甲基氨基）丙基] -3-乙基碳二亚胺盐酸盐，1- [3-（二甲基氨基） 丙基] -3-乙基碳二亚胺，1,3-二异丙基碳二亚胺或1,3-二环己基碳二亚胺。
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公开(公告)号：KR1020120067819A
公开(公告)日：2012-06-26
申请号：KR1020100129430
申请日：2010-12-16
Applicant: 동화약품주식회사
IPC: C07D403/10 , A61K31/4184 , A61K31/4178 , A61P9/12
CPC classification number: Y02P20/55 , C07D403/10 , A61K31/4184
Abstract: PURPOSE: An improved method for preparing candesartan cilexetil is provided to simplify entire process under a mild condition. CONSTITUTION: A method for preparing candesartan cilexetil of chemical formula 1 comprises: a step of dissolving a compound of chemical formula 2 in a dichloromethane solution; a step of adding a mixture solution of alcohol and acetyl chloride to the dichloromethane solution; a step of deprotecting to remove triphenyl methane protection groups and obtain a compound of chemical formula 1; a step of adding ethyl acetate and n-hexane and precipitating the compound of chemical formula 1.
Abstract translation: 目的：提供一种改进的坎地沙坦替卡西汀的制备方法，以简化温和条件下的整个过程。 构成：制备化学式1的坎地沙坦酯的方法包括：将化学式2的化合物溶解在二氯甲烷溶液中的步骤; 将醇和乙酰氯的混合溶液加入到二氯甲烷溶液中的步骤; 去除三氯甲烷保护基并脱除化学式1化合物的步骤; 加入乙酸乙酯和正己烷并使化学式1的化合物沉淀的步骤。
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