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

被引:26
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
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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页码:967 / 975
页数:9
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