公开(公告)号：KR100475244B1

公开(公告)日：2005-03-10

申请号：KR1020020036636

申请日：2002-06-28

Applicant: 한국화학연구원

Inventor： 김문환 ,  심영기 ,  이광재 ,  이수헌 ,  류의상 ,  안승호

IPC: C07C231/12

Abstract: 본 발명은 아토르바스타틴(상품명:리피토)을 제조하기 위한 핵심 중간체인, 4-(4-플루오르페닐)-2-이소부티릴-3-페닐-4-옥소-
N -페닐-부티르아미드의 효율적인 제조방법에 관한 것으로서, 4-메틸-3-옥소-
N -페닐펜타미드와 2-할로-1-(4-플루오르페닐)-2-페논 또는 2,2-디할로-1-(4-플루오르페닐)-2-페논을 염기 존재 하에서 친핵성 치환반응시키는 본 발명에 따르면 온화한 조건에서 높은 수율로 아트로바스타틴 제조용 중간체를 수득할 수 있다.

公开(公告)号：KR1020040001435A

公开(公告)日：2004-01-07

申请号：KR1020020036636

申请日：2002-06-28

Applicant: 한국화학연구원

Inventor： 김문환 ,  심영기 ,  이광재 ,  이수헌 ,  류의상 ,  안승호

IPC: C07C231/12

Abstract: PURPOSE: Provided is a method for preparing an atorvastatin synthetic intermediate, 4-(4-fluorophenyl)-2-isobutyryl-3-phenyl-4-oxo-N-phenylbutyramide under a mild condition in a short time by a simple process at a high yield and with a high purity. CONSTITUTION: The method for preparing 4-(4-fluorophenyl)-2-isobutyryl-3-phenyl- 4-oxo-N-phenylbutyramide represented by the formula 2 comprises the step for carrying out the nucleophilic substitution reaction of 4-methyl-3-oxo-N-phenylpentamide represented by the formula 3 with 2-halo-1-(4-fluorophenyl)2-phenone represented by the formula 4 or 2,2-dihalo-1- (4-fluorophenyl)-2-phenone represented by the formula 5, or the mixture thereof in the presence of a base, wherein X is Cl, Br or I.

Abstract translation: 目的：提供一种在短时间内通过简单方法在温和条件下制备阿托伐他汀合成中间体4-（4-氟苯基）-2-异丁酰基-3-苯基-4-氧代-N-苯基丁酰胺的方法， 高产量和高纯度。 构成：由式2表示的4-（4-氟苯基）-2-异丁酰基-3-苯基-4-氧代-N-苯基丁酰胺的制备方法包括进行4-甲基-3的亲核取代反应的步骤 由式3代表的2-卤代-1-（4-氟苯基）-2-苯酮或2,2-二卤代-1-（4-氟苯基）-2-苯酮代表的由式3表示的2-氧代-N-苯基戊酰胺代表 通式5，或其在碱存在下的混合物，其中X为Cl，Br或I.