Wyeth

Ayman Sahli

George Anello Chiarello

Chunhao Zhang

Anthony Pilcher

Adam P Michaud

Clifford William Coughlin

James S Farina

A method is disclosed for preparing hydrazides from hydrazine and an acyl chloride which comprises the steps of (a) preparing a stirred substantially uniform slurry comprising hydrazine and an inert solvent at low temperature; and (b) adding an acyl chloride continuously to said slurry. The method avoids or limits production of undesired bis-hydrazide by-products. The method is used to prepare 3-methyl-3-mercaptobutanoic acid hydrazide, a molecule used to link calicheamicin to a monoclonal antibody.

Processes for making hydrazides

A scalable process for the preparation of a rapamycin 42-ester by reacting a rapamycin 42-ester boronate with a diol and purifying crude rapamycin 42-ester by recrystallization and treatment with a diol is provided. Also provided is a method for isolating and purifying a rapamycin 42-ester boronate from mother liquors comprising acetone and rapamycin contaminants.

Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate

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Amman, Jordan

Ayman Sahli