公开(公告)号：US20190233456A1

公开(公告)日：2019-08-01

申请号：US16337338

申请日：2017-09-19

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Hong LIU ,  Jiang WANG ,  Shengbin ZHOU ,  Panfeng PENG ,  Yong NIAN ,  Shuni WANG ,  Shuangjie SHU ,  Hao SHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07F15/04 ,  C07D207/16

CPC classification number: C07F15/045 ,  C07C227/34 ,  C07C229/34 ,  C07D207/16 ,  C07D401/04 ,  C07D409/12 ,  C07F15/04 ,  Y02P20/55

Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.

公开(公告)号：US20170044187A1

公开(公告)日：2017-02-16

申请号：US15109101

申请日：2014-12-29

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Hong LIU ,  Beili WU ,  Yongtang ZHENG ,  Xin XIE ,  Hualiang JIANG ,  Panfeng PENG ,  Ronghua LUO ,  Jing LI ,  Jian LI ,  Ya ZHU ,  Ying CHEN ,  Haonan ZHANG ,  Liumeng YANG ,  Yu ZHOU ,  Kaixian CHEN

IPC: C07D519/00 ,  C07D451/04 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D519/00 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  C07D451/04 ,  A61K2300/00

Abstract: Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

Abstract translation: 提供由式（I）表示的1-（3-氨基丙基）取代的环胺化合物，其药学上可接受的盐，对映体，非对映异构体，外消旋体及其混合物，以及合成所述1-（3-氨基丙基）取代的环胺 化合物采用芳香族杂环甲醛为原料。 所述化合物可用作治疗HIV感染的CCR5拮抗剂。