公开(公告)号：US20040176441A1

公开(公告)日：2004-09-09

申请号：US10798131

申请日：2004-03-11

Applicant: Mars Incorporated

Inventor： Leo J. Romanczyk JR. ,  Amit Basak ,  Craig A. Townsend

IPC: C07D45/14 ,  A61K031/353

CPC classification number: C07D311/32 ,  Y02P20/55

Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having nullnnull procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4null8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8null8), (8null6), and (6null6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (null)-epicatechin is produced under certain conditions.

Abstract translation: 公开了用于生产具有“n”原花青素单体单元（其中n为2至18）的直链和支链原花青素低聚物的方法。该方法包括将保护的活化单体与未保护的单体偶联以产生部分保护的（4-> 8）二聚体 。 将二聚体任选地封闭，与活化的受保护的单体偶联以产生部分保护的，任选被封闭的三聚体并脱保护。 可以重复这些步骤以产生更高级的低聚物。 还提供了制备（8-> 8），（8-> 6）和（6-> 6）二聚体和双支链低聚物的方法。 在某些条件下制备8-溴四-O-苄基（ - ） - 表儿茶素的结晶。

公开(公告)号：US20030114691A1

公开(公告)日：2003-06-19

申请号：US10212973

申请日：2002-08-06

Applicant: Mars Incorporated

Inventor： Leo J. Romanczyk JR. ,  Amit Basak ,  Craig A. Townsend

IPC: C07D313/00

CPC classification number: C07D311/32 ,  Y02P20/55

Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having nullnnull procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4null8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8null8), (8null6), and (6null6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (null)-epicatechin is produced under certain conditions.

Abstract translation: 公开了用于生产具有“n”原花青素单体单元（其中n为2至18）的直链和支链原花青素低聚物的方法。该方法包括将保护的活化单体与未保护的单体偶联以产生部分保护的（4-> 8）二聚体 。 将二聚体任选地封闭，与活化的受保护的单体偶联以产生部分保护的，任选被封闭的三聚体并脱保护。 可以重复这些步骤以产生更高级的低聚物。 还提供了制备（8-> 8），（8-> 6）和（6-> 6）二聚体和双支链低聚物的方法。 在某些条件下制备8-溴四-O-苄基（ - ） - 表儿茶素的结晶。