NOVEL 100ALPHA*111ALPHAAMETHYLENEE PROSTAGLADINE AND PROCESS FOR PREPARING SAME*

Japanese Patent JPS51125369

A

Process for the preparation of 10 α, 11 α -methylene-prostaglandins of the general formula i ** (see formula) ** Wherein r1 represents one of the groupings -or5, -nhso2ch3 or -o-ch2-uv, wherein r5 signifies a hydrogen atom, an alkyl, aryl or heterocyclic group, u means a direct bond, a carbonyl or carbonyloxy group, and v represents a phenyl ring substituted with one or more phenyl groups, alkoxy groups of 1 to 2 carbon atoms or halogen atoms, preferably bromine atoms; r2 means a hydrogen atom or an alkyl group of 1 to 5 carbon atoms; r3 means an alkyl group, a substituted or unsubstituted cycloalkyl group, an straight or branched chain alkyl group of 1 to 5 carbon atoms substituted with optionally substituted aryl, an optionally substituted aryl group, a benzodioxol-2-yl group; r4 represents a hydrogen atom or an ether or acyl radical; and r6 signifies a hydrogen atom or an alkyl group of 1 to 3 carbon atoms; a means a group -ch2-ch2 or a group cis-ch = ch-; b means a group -ch2-ch2 or a group trans-ch = ch-; d and e together signify a direct link; or d means an straight or branched chain alkyl group of 1 to 5 carbon atoms and e means an oxygen or sulfur atom; and z means a carbonyl group or a group (see formula) whose radical or4 may be in position α-; - or β and, if r1 represents a hydroxy group, its salts physiologically compatible with bases, characterized in that a compound of the general formula ii is subjected to methyleneization. ** (see formula) ** Where a, b, d, e, r1, r2, r3 and r4 have the meanings indicated above, and then, depending on the desired end-of-account meaning of r1, a, b, d, e and z in the final product, in any order of succession, an esterified 1-carboxy group is saponified or a free 1-carboxy group is esterified and/or a 9-keto group is reduced, and/or a double bond is hydrogenated in position 5,6 and/or a double bond is hydrogenated at positions 5,6 and 13,14; and/or a free oh group is functionally transformed; and/or a functionally modified oh group is released; and optionally a 1-carboxy group, with a base, is transformed into the physiologically compatible salt, and optionally the racemates are split.

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HERUMUUTO FUORUBURIYUTSUGEN
BERUNTO RADEYUTSUHIERU
BERUNAA SUKUBARA
GERUDA MANNESUMAN
BARUTAA ERUGAA

JP2904476A

November 01, 1976

March 17, 1976

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SCHERING AG

A61K31/21; C07C67/00; C07C401/00; C07C405/00; A61K31/185; (IPC1-7): A61K31/185; A61K31/215; C07C61/38; C07C69/74; C07C69/95; C07C145/00; C07C149/26

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