Process for preparing acid addition salt of Z-isomer of tripheny

Details Process for preparing acid addition salt of Z-isomer of tripheny Process for preparing acid addition salt of Z-isomer of tripheny

1995-06-06

1996-10-15

Raymond, Richard L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

544174, 544396, 546236, 548575, 558414, 560 58, 560101, 560142, 560133, C07C21310

Patent

active

055656110

ABSTRACT:
The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.5 represents a lower alkyl group or halo; and n represents 1-6, characterized in that the E-isomer of the compound of the formula (I) or its acid addition salt, singly or in admixture with the Z-isomer or its acid addition salt, is heated in an organic solvent containing hydrobromic acid.

REFERENCES:
patent: 4960937 (1990-10-01), Woschina et al.
patent: 4973755 (1990-11-01), Grafe et al.
J. Synth. Org. Chem., 1987, pp. 816-817, Mohammed I. Al-Hassan, A Single-Step Synthesis of Tamoxifen Using Palladium-Catalyzed Cross Coupling.
Synth. Commun., 1987, pp. 1247-1251, Mohammed I. Al-Hassan, Synthesis of cis-and trans-tamoxifen, punlished on 1987, U.S.
J. Chem. Soc. Perkin Trans. II 1988, "The Role of the 2-Methyl Substituent in Governing Stereoselective Formation of the E Isomer in the Synthesis of 4-Hydroxy-2-methyltamoxifen (1-{4-[2-(Di-methylamino)ethoxy]phenyl}-1-(4-hydroxy-2-methylphenyl)-2phen ylbut-1-ene)", Raymond McCague et al, pp. 1201-1208.
Chemical Abstract, vo. 118, 1993, p. 842, Abstract No. 118:254522g, "Preparation of tamoxifen citrate without separation of the geometric isomers".

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