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K. B. Hansen, J. Balsells, S. Dreher, Y. Hsiao, M. Kubryk, M. Palucki, N. Rivera, D. Steinhuebel, J. D. Armstrong III, D. Askin and E. J. Grabowski, “First Generation Process for the Preparation of the DPP-IV Inhibitor Sitagliptin,” Organic Process Research & Development, Vol. 9, No. 5, 2005, pp. 634-639. doi:10.1021/op0500786

has been cited by the following article:

• TITLE: Solid Phase Synthesis of 3,4,5-Trisubstituted-1,2,4-Triazoles Derivatives from the Resin-Bound Acylhydrazines

  AUTHORS: Rongjian Xie, Xingang Liu, Chao Mai, Zhanxiang Liu

  KEYWORDS: Resin-Bound Acylhydrazine; Solid-Phase Synthesis; 1, 2, 4-Triazoles

  JOURNAL NAME: International Journal of Organic Chemistry, Vol.3 No.1A, April 30, 2013

  ABSTRACT: An extension of our methodology on solid-phase synthesis of 3,4,5-trisubstituted-1,2,4-triazoles under mild conditions has been developed. Firstly, the resin-bound acylhydrazine is reacted with orthoesters to provide resin-bound 1,3,4-oxadiazoles. Secondly, condensation of 1,3,4-oxadiazoles resin with the corresponding arylamines hydrochloride to form the the resin-bound triazoles. 3,4,5-Trisubstituted-1,2,4-triazoles derivatives were obtained from resin-bound acylhydrazines in several steps providing 78% - 87% overall yields and excellent purity. The advantages of this method include straightforward operation and high yield and purity of the products.