| WARF: P95154US |  |
| 20-Epi-19-Nor-Vitamin D Compounds |
| INVENTORS | • | Hector DeLuca, Heinrich Schnoes, Fariba Aria |
OVERVIEW
A synthesis of 1 alpha-hydroxy-19-nor-vitamin D compounds comprises (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7 E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.
ADDITIONAL INFORMATION
Intellectual Property Status
Patent applied for.
Tech Fields
Pharmaceuticals & Vitamin D - Vitamin D
CONTACT INFORMATION
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