METHOD FOR PREPARING 7α-METHYLSTEROIDS, COMPOUND Russian patent published in 2007 - IPC C07J51/00 C07J1/00 C07J5/00 

Abstract RU 2305105 C2

FIELD: organic chemistry, steroids, chemical technology.

SUBSTANCE: invention relates to an improved method for synthesis of 7α-methylsteroids of the general formula (I) wherein R1 means hydrogen atom (-H), -CH3 or -C≡CH; R2 means -(CH2)nOH wherein n = 0, 1 or 2. Method involves using copper (Cu(II) acetate or chloride preferably), 1,6-coupled addition of Grignard reagent of the formula CH3MgX wherein X means halogen atom to 4,6-unsaturated 3-ketosteroid of the formula (II) wherein r1 and R2 have above given values and wherein hydroxy-group of steroid of the formula (II) is protected by trialkylsilyl group followed by its treatment with Grignard reagent and removal of a protective group. Method enhances stereoselectivity by the yield of 7α-isomer.

EFFECT: improved method of synthesis.

18 cl, 3 ex

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RU 2 305 105 C2

Authors

Stulvinder J.

Ostendorf M.

Bjugenjum Van P.A.M.

Dates

2007-08-27Published

2003-01-14Filed