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��ѧ��ҵ�빤�� 2005, Vol. 22 Issue (5) :354-357    DOI:
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Stereoselectivity of Acetalization in Synthesis of Budesonide
XU Li-ying, WANG Dong-hua(College of Pharmaceutical Science & Technology, Tianjin University, Tianjin 300072, China)
(College of Pharmaceutical Science & Technology, Tianjin University, Tianjin 300072, China

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Abstract�� The last step of Budesonide synthesis is acetalization of 16��-hydroxyprednisolone with n-butyraldehyde while a chiral 22-C is newly formed.Currently the marketed product is approximately a 1��1(molar ratio) mixture of the two diastereoisomers, 22R and 22S.Since later studies demonstrated therapeutic superiority of R over S, studies were launched here with an aim to raise the ratio of R in the product.Results showed that at 25 �� with perchloric acid as catalyst in dichloromethane for 3 h, a 96% yield of a product containing 22R to 22S as 85��15(molar ratio) was obtained.
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Received 2005-09-15; published 2005-09-15
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����ӱ,������.�����εºϳ�����ȩ��Ӧ������ѡ����[J].  ��ѧ��ҵ�빤��, 2005,22(5): 354-357
XU Li-ying, WANG Dong-hua.Stereoselectivity of Acetalization in Synthesis of Budesonide[J].  Chemcial Industry and Engineering, 2005,22(5): 354-357
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