Radical-mediated intramolecular β-C(sp3)-H amidation of alkylimidates: Facile synthesis of 1,2-amino alcohols
A new radical-mediated intramolecular β-C(sp3)-H amidation reaction of O-alkyl trichloro- or arylimidates is reported. Various oxazolines were efficiently prepared from easily accessible alcohol starting materials. The trichloro-oxazoline products can be hydrolyzed under mild conditions to give valuable 1,2-amino alcohols. This amidation reaction exhibits a broad substrate scope and good functional group tolerance, and offers a powerful means for the C(sp3)-H functionalization of alcohols. Mechanistic studies suggest that a sequence of 1,5-HAT of an imidate radical, iodination and cyclization might be operative.
Mou, Xue-Qing,Chen, Xiang-Yu,Chen, Gong,He, Gang
supporting information
p. 515 - 518
(2018/01/19)
PROCESS FOR THE PREPARATION OF (S)-2-AMINO-1-PROPANOL (L-ALANINOL) FROM (S)-1-METHOXY-2-PROPYLAMINE
The invention relates to a process for the preparation of (S)-2-amino-1-propanol (L-alaminol) from (S)-1-methoxy-2-propylamine via the hydrochloride of (S)-2-amino-1-propanol and subsequent work-up.
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Page/Page column 3
(2010/10/03)
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