公开(公告)号：US20180251428A1

公开(公告)日：2018-09-06

申请号：US15756267

申请日：2016-08-10

Applicant: Merck Patent GmbH

Inventor： Luc EBERHARDT ,  Andreas WAECHTLER ,  David MAILLARD ,  Stefan LEHMANN

IPC: C07D217/14 ,  B01J31/12 ,  C07D401/04 ,  B01J31/24

CPC classification number: C07D217/14 ,  B01J31/122 ,  B01J31/2409 ,  B01J31/2452 ,  B01J31/249 ,  B01J2531/0266 ,  B01J2531/827 ,  C07B53/00 ,  C07D401/04

Abstract: The present invention provides methods of preparing Praziquantel, in particular (R)-Praziquantel and analogues thereof in a stereoselective manner. One method involves asymmetric hydrogenation of the following intermediate compound and subsequent cyclization.

公开(公告)号：US20180155339A1

公开(公告)日：2018-06-07

申请号：US15528282

申请日：2015-11-17

Applicant: MERCK PATENT GMBH

Inventor： Andreas WAECHTLER ,  Hadia SALEH-KASSIM ,  Christian JASPER ,  Joern KOLB ,  David MAILLARD

IPC: C07D471/04 ,  C07B55/00 ,  C07B57/00 ,  C07C31/30

CPC classification number: C07D471/04 ,  C07B55/00 ,  C07B57/00 ,  C07B2200/07 ,  C07C31/30

Abstract: The present invention relates to a method for the racemization of enantiomerically pure or enantiomerically enriched Praziquantel under basic conditions and a method for the production of (R)-Praziquantel in enantiopure or enantiomerically enriched form, which comprises the racemization method.

公开(公告)号：US20170320873A1

公开(公告)日：2017-11-09

申请号：US15528116

申请日：2015-11-19

Applicant: Merck Patent GmbH

Inventor： David MAILLARD ,  Andreas WAECHTLER ,  Jeremy MAURIN ,  Ewgenij WAKARESKO ,  Christian JASPER

IPC: C07D471/04 ,  C07C59/84 ,  C07C59/64 ,  C07D217/14

CPC classification number: C07D471/04 ,  C07B2200/07 ,  C07C59/64 ,  C07C59/84 ,  C07D217/14

Abstract: The present invention relates to methods for the production of enantiopure or enantioenriched Praziquantel precursors and to methods for the production of enantiopure or enantioenriched Praziquantel comprising the methods for the production of the Praziquantel precursors. The present invention further relates to compounds or intermediates useful in such methods.