An improved and scalable process for 3,8-diazabicyclo[3.2.1]octane analogues

Autor:	Da Wei Teng, Long Jiang Huang
Rok vydání:	2011
Předmět:	chemistry.chemical_compound Benzylamine chemistry Process development Yield (chemistry) Diol Organic chemistry General Chemistry Combinatorial chemistry Octane
Zdroj:	Chinese Chemical Letters. 22:523-526
ISSN:	1001-8417
DOI:	10.1016/j.cclet.2010.11.030
Popis:	An improved and scalable process for substituted 3,8-diazabicyclo[3.2.1]octane was developed. N-Benzyl-2,5-dicarbethoxy-pyrrolidine 2 was reduced to N-benzyl-2,5-dihydroxymethylpyrrolidine 9 and subsequently debenzylated to afford N-Boc-2,5-dihydroxymethylpyrrolidine 10. After mesylation of the diol 10 and cyclization with benzylamine, a diversity of scaffold, 3,8-diazabicyclo[3.2.1]octane analogue 12 was obtained in a total yield of 42% in five steps.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::cbc8fe6d9c9e39d37201bdc95642b6ac https://doi.org/10.1016/j.cclet.2010.11.030 Zobrazit plný text záznamu Full Text from ScienceDirect