期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 64, 期 7, 页码 704-717出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c15-00983
关键词
aza-Michael addition; alpha,beta-unsaturated carboxylic acid; integrated catalyst; thiourea; arylboronic acid; O-benzylhydroxylamine
资金
- Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan [23105007]
- Grants-in-Aid for Scientific Research [16H06384, 16H02604] Funding Source: KAKEN
The first intermolecular asymmetric Michael addition of nitrogen-nucleophiles to alpha,beta-unsaturated carboxylic acids was achieved through a new type of arylboronic acid equipped with chiral aminothiourea. The use of BnONH2 as a nucleophile gives a range of enantioenriched beta-(benzyloxy)amino acid derivatives in good yields and with high enantioselectivity (up to 90% yield, 97% enantiomeric excess (ee)). The obtained products are efficiently converted to optically active beta-amino acid and 1,2-diamine derivatives.
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