The author of 《Identification of dihydrofuro[3,4-d]pyrimidine derivatives as novel HIV-1 non-nucleoside reverse transcriptase inhibitors with promising antiviral activities and desirable physicochemical properties》 were Kang, Dongwei; Zhang, Heng; Wang, Zhao; Zhao, Tong; Ginex, Tiziana; Luque, Francisco Javier; Yang, Yang; Wu, Gaochan; Feng, Da; Wei, Fenju; Zhang, Jian; De Clercq, Erik; Pannecouque, Christophe; Chen, Chin Ho; Lee, Kuo-Hsiung; Murugan, N. Arul; Steitz, Thomas A.; Zhan, Peng; Liu, Xinyong. And the article was published in Journal of Medicinal Chemistry in 2019. Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate The author mentioned the following in the article:
To address drug resistance to HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel diarylpyrimidine (DAPY) derivatives targeting “”tolerant region I”” and “”tolerant region II”” of the NNRTIs binding pocket (NNIBP) were designed utilizing a structure-guided scaffold-hopping strategy. The dihydrofuro[3,4-d]pyrimidine derivatives I and II proved to be exceptionally potent against a wide range of HIV-1 strains carrying single NNRTI-resistant mutations (EC50 = 0.9-8.4 nM), which were remarkably superior to that of etravirine III. Meanwhile, both compounds exhibited comparable activities with III toward the virus with double mutations F227L+V106A and K103N+Y181C. Furthermore, the most active compound I showed favorable pharmacokinetic properties with an oral bioavailability of 30.96% and a half-life of 11.1 h, which suggested that I is worth further investigation as a novel NNRTI to circumvent drug resistance. In the experiment, the researchers used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate)
tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem