METHOD FOR PRODUCTION AND PURIFICATION OF MISOPROSTOL Russian patent published in 2022 - IPC C07C67/347 C07C67/56 C07C69/738 C07F1/02 C07F1/08 

Abstract RU 2774634 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to a method for the production of a compound of the general formula I,

,

where R is C1-4alkyl group with a straight or branched chain. The method consists in combination of vinylcuprate of the general formula II, which is obtained by means of reaction of vinylstannane of the general formula III with copper halogenide of the general formula CuX and alkyl lithium R1Li,

,

where R2 is H or a protective group for an alcohol group, optionally containing a silicon atom, or a cyclic or acyclic alkyl group containing an oxygen atom; X is a iodine atom or a bromine atom, R1 is C1-6alkyl group, n >2, if R2 differs from a hydrogen atom, n>3, if R2 is a hydrogen atom, with protected enon of the general formula IV,

,

where R3 is THP- or trialkyl silyl group, and has R value defined above. At the same time, excessive alkyl lithium, which is used relatively to copper halogenide CuX, in case if R2 ≠ H, at molar ratio of 2-2.4, in case if R2 = H, at a molar ratio of 3-3.4, is decomposed before the reaction of combination of compounds of the general formula II and IV, protective groups of the resulting compound of the general formula V are removed,

,

where values R, R2 and R3 are defined above, and the resulting compound of the general formula I is purified using chromatography.

EFFECT: significant reduction in the number of impurities at the output of a combination reaction.

16 cl, 5 ex

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RU 2 774 634 C2

Authors

Hortobagyi, Iren

Laszlofi, Istvan

Kardos, Zsuzsanna

Molnar, Jozsef

Takacs, Laszlo

Horvath, Kornelia

Dates

2022-06-21Published

2018-06-29Filed