A convenient and practical synthesis of imidazol-1-yl-acetic acid hydrochloride was achieved via N-alkylation of imidazole using tert-butyl chloroacetate followed by a non-aqueous ester cleavage of the resulting imidazol-1-yl-acetic acid tert-butyl ester in the presence of titanium tetrachloride. The synthesized imidazol-1-yl-acetic acid hydrochloride was then utilized to prepare zoledronic acid.

An alternative and practical synthesis of (S)-1-(2-chloroacetyl)pyrrolidine-2-carbonitrile was achieved. Reaction of L-proline with chloroacetyl chloride was followed by conversion of the carboxylic acid moiety of the resulting N-acylated product into the carbonitrile via the corresponding amide intermediate. The synthesized pyrrolidine derivative was utilized to prepare DPP-IV inhibitor Vildagliptin.

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Peptides U 0400 Concise and Efficient Synthesis of Highly Potent and Selective Dipeptidyl Peptidase II Inhibitors. -A more practical, shorter, high yielding route for the synthesis of the highly potent and selective DPP II inhibitors (IX) and (XII) starts from L-glutamine. -(RASHEED*, M. A.; NAMALA, R.; MANNE, N.; VANJIVAKA, S.; DHAMJEWAR, R.; BALASUBRAMANIAN, G.; Synth. Commun. 38 (2008) 2, 162-169; GVK Biosci., IDA, Hyderabad 500 076, India; Eng.) -H. Toeppel 26-192