Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 11, Issue 2, Pages 200-205Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op060130d
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1 alpha,25-Dihydroxyvitamin D-3 (calcitriol) 1 and synthetic analogues thereof are highly potent compounds with a wide range of pharmacological activity making them of great interest for the pharmaceutical industry. Herein we report an improved synthesis of the calcitriol analogue 2, which features a novel oxazole-containing side chain. The crucial part of the synthesis was the development of a practical route to the beta-keto phosphonate 28, allowing an easy introduction of the unnatural side chain by a Wittig Horner reaction.
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