AbstractA novel one-pot, multicomponent asymmetric synthesis of α-amidosulfides was described. By employing chiral phosphoric acid as Brønsted acid and catalyst, α-amidosulfides were obtained in excellent yields with high to excellent enantioselectivities via reaction of thiophenol and N-acylimines generated in situ from α-amidosulfones. Graphical abstract
Efficient Synthesis of N-Carbamoylpropargylamines from α-Amido Sulfones Using Dimethylalkynylaluminum Reagents
作者:Sang-Hyeup Lee、Ji-Hoon Lee
DOI:10.1055/s-0041-1737763
日期:2022.5
reagents derived from terminal alkynes and trimethylaluminum underwent addition to various N-activated α-amidosulfones to produce the corresponding alkynylamines in moderate to excellent yields. The optimized protocol avoids the preparation and isolation of relatively unstable N-activated imines that are generated in situfrom their corresponding, stable, N-activated α-amidosulfones. This methodology
Process for the preparation of a 1,3-oxazolidine-5-carboxylic acid
申请人:Rhone-Poulenc Rorer, S.A.
公开号:US05811550A1
公开(公告)日:1998-09-22
Method for the preparation of 1,3-oxazolidin 5-carboxylic acid having the general formula (I) ##STR1## from a product having the general formula (II) ##STR2## In the general formulas (I) and (II), Ar is an aryl radical, R.sub.1 is a benzoyl radical or a radical R.sub.2 --O--CO-- wherein R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, Ph is an optionally substituted phenyl radical, X is the residue of an optically active organic base or an alkoxy radical optionally substituted by a phenyl radical. The acids of formulas (I) and (II) are particularly useful in preparing taxol, Taxotere or analogs thereof which have remarkable antitumor and antileukemia properties.