Sandoz Gmbh

Sandoz Pharm. Corp.

Jerome Linder

William J Houlihan

Goetz E Hardtmann

Prasad Koteswara Kapa

Sompong Wattanasin

George T Lee

Kau-Ming Chen

An improved process for preparing glycine hydrochloride in a high purity and high yield employing water as the solvent.

Process for preparing glycine hydrochloride

Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, and

Processes for the synthesis of diprotected

The .alpha.,.alpha.-dibromo-substituted or unsubstituted-4-pivaloyl toluenes, e.g., .alpha.,.alpha.-dibromo-4-pivaloyl toluene, are prepared by bromination of a corresponding p-pivaloyl toluene with liquid bromine at a temperature of at least 125.degree. C.

Dibromination process

Substituted 5-hydrazinopyridazin-3(2H)-ones, e.g., 4-chloro-2-(3-trifluoromethylphenyl)-5-(1-methylhydrazino)-pyridazin-3(2H) -one or 4-chloro-2-(2-fluoro-5-trifluoromethylphenyl)-5-(1-methylhydrazino)-pyrida zin-3(2H)-one, are prepared by treating halogenated pyridazin-3-(2H)-ones with hydrazine and substituted hydrazines and are useful as central nervous system depressants and sleep inducers.

5-Hydrazinopyridazin-3(2H)-ones

The .alpha.-bromo-substituted or unsubstituted-4-pivaloyl toluenes, e.g., .alpha.-bromo-4-pivaloyl toluene, are prepared by bromination of a corresponding p-pivaloyl toluene with liquid bromine at a temperature of at least 100.degree.C.

Bromination process

Disclosed is single phase multi-stage process for preparation of 1-aryl-4,5-dihalo-pyridazones-6 involving the diazotization of an amino aryl compound, e.g. aniline, followed by reduction with sulfurous acid to obtain the corresponding aryl hydrazine which is then reacted at elevated temperatures with a mucohalic acid to obtain the 1-aryl-4,5-dihalo-pyridazone-6.

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Westfield, NJ, United States of America

Jerome Linder