Development of an Improved Process for Doxercalciferol via a Continuous Photochemical Reaction

被引：27

作者：

Anderson, Bruce G. ^{[1
]}

Bauta, William E. ^{[1
]}

Cantrell, William R., Jr. ^{[1
]}

机构：

[1] Genzyme Corp, San Antonio, TX 78245 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2012年 / 16卷 / 05期

关键词：

VITAMIN-D ANALOG; ERGOCALCIFEROL VITAMIN-D2; HYDROXYLATION; DEGRADATION; D-3;

D O I：

10.1021/op200346g

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Doxercalciferol (1 alpha-hydroxyvitamin D2) is a commercially approved vitamin D derivative used to treat chronic kidney disease (CKD) patients whose kidneys cannot metabolically introduce a hydroxyl group at C1. A new process for the production of doxercalciferol from ergocalciferol was developed using a continuous photoisomerization of a known vitamin D intermediate as the key step, thus circumventing the limitations of batch photoisomerization processes. Doxercalciferol is produced in an overall yield of about 10% from ergocalciferol.

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收藏

页码：967 / 975

页数：9

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