7α-メチルステロイドの調製方法

Japanese Patent JP5250174

B2

The invention relates to a process for the preparation of 7α-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C≡CH; R2 is (CH2)nOH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Grignard reagent CH3MgX, X being a halogen, to the 4,6-unsaturated 3-ketosteroid of formula II, wherein R1 and R2 are as previously defined, comprising protecting the hydroxy group of the steroid of formula II with a trialkylsilyl group, followed by treating the hydroxy protected steroid with the Grignard reagent. The process of the invention is useful for the production of pharmacologically interesting steroids.

JP3466651	NEW STEROID HAVING METHYLENE LACTONE GROUP ON 17-TH POSITION, ITS PRODUCTION, ITS INTERMEDIATE, ITS USE AS PHARMACEUTIC, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
WO/2002/069977	USE OF CERTAIN STEROIDS FOR TREATMENT OF BLOOD CELL DEFICIENCIES
WO/2002/076465	OESTROGEN AND FATTY ACID MONOESTER AS A HYPOLIPIDAEMIC AND ANTIDIABETIC AGENT

St Elbindel, Yeh
Ostendorff, M
Bhunam, Juan Pare A M

JP2003560033A

July 31, 2013

January 14, 2003

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STICHTING TOP INSTITUTE PHARMA

C07J1/00; C07J5/00; C07J7/00; C07J51/00

US3341557
WO2001058919A2
WO2001005806A1
WO2000059920A2

CAMPBELL,J.A. et al.,7α-Methyl-18-norsteroids:A new class of potent anabolic and androgenic hormones,Steroids,Vol.1,No.3,pp.317-324(1963)
NICKISCH,K. et al.,Stereoselektive synthese von 7α-alkyl und 7α-propylsteroiden ,Tetrahedron Letters,1988年,Volume 29,Issue 13,Pages 1533-1536

Kawaguchi International Patent Office
Chihiro Watanabe
Katsuma Osaki
Mitsuaki Tsubokura

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