Pfizer Corporation

Robert J Sysko

Douglas J Allen

Terry G Sinay

Raymond C Glowaky

Terry Gene Sinay, Jr

Steven R Kurowsky

This invention relates to a novel crystalline polymorphic form of sertraline hydrochloride, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4 -tetrahydro-N-methyl-1-naphthalenamine hydrochloride, and to a method for preparing it.

Sertraline polymorph

This invention relates to a process for the production of phthalazineacetic acid ester derivatives of the formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl which comprises reacting (Z)-3-oxo-1(3H)-isobenzofuranylideneacetic acid with hydrazine in the presence of a solvent; reacting the resulting mixture of the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid and 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of a solvent; and reacting the resulting 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of an alcohol. This invention also relates to the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid of the formula ##STR2## which is an intermediate formed in the process of this invention and which is useful for the production of phthalazineacetic acid ester derivatives of formula IV. The compounds of formula IV are useful for the preparation of certain heterocyclic oxophthalazinyl acetic acids and esters thereof.

Process for the production of phthalazineacetic acid ester derivatives

This invention relates to a process for the production of phthalazineacetic acid ester derivatives of the formula ##STR1## wherein R is (C.sub.1 -C.sub.4) alkyl which comprises reacting (Z)-3-oxo-1(3H)-isobenzofuranylideneacetic acid with hydrazine in the presence of a solvent; reacting the resulting mixture of the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid and 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of a solvent; and reacting the resulting 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of an alcohol. This invention also relates to the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid of the formula ##STR2## which is an intermediate formed in the process of this invention and which is useful for the production of phthalazineacetic acid ester derivatives of formula IV. The compounds of formula IV are useful for the preparation of certain heterocyclic oxophthalazinyl acetic acids and esters thereof.

An improved process for making 6,6-diiodopenicillanic acid, an intermediate for preparation of 6-beta-iodopenicillanic acid, a beta-lactamase inhibitor, which comprises diazotizing 6-beta-aminopenicillanic acid in the presence of iodine, followed by washing the product of said process with an aqueous solution of an alkali metal iodide.

Pure 6,6-diiodopenicillanic acid and process for its preparation

Amine polymers are used to dewater suspensions of particulate matter in water. The polymers are synthesized by the reaction of a nitrile polymer such as polyacrylonitrile, an aminating agent, and a sulfur activator. The dewatering properties of these amine polymers can be beneficially employed to treat sewage sludge, silt laden water, industrial waste and the like.

Growing community of inventors

Niantic, CT, United States of America

Robert J Sysko