Abstract: A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: A process is provided for preparing the intermediate A in accordance with the following reaction sequence The intermediate A is used in preparing DPP IV inhibitors which are useful in treating diabetes.

Abstract: A process is provided for preparing the dipeptidyl peptidase of the structure I (also referred to as saxaglipitin) by direct dehydration, in one pot, of the amide II by reacting amide II with phosphorus oxychloride in an organic solvent such as dichloromethane, quenching the reaction mixture with water to form the hydrochloric acid salt of I, and treating the hydrochloric acid salt with base to form the free base of I.

Abstract: A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure wherein is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reagent and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicarbonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.

Abstract: Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate.