86052-28-0Relevant articles and documents
PO-Activated Olefination and Conversion of Aldehydes and Ketones to Higher Amines; II. Synthesis of Arylethylamines
Heymes, A.,Chekroun, I.
, p. 245 - 249 (2007/10/02)
The transformation of arylcarboxaldehydes and/or - ketones 2 by three different routes into arylethylamines 3 and/or 4 is reported.According to the first route, the intermediate iminophosphonates 9 react through a classical PO-activated olefination.The second and the third involve the rearrangement of the iminophosphonates 9 into the vinylphosphoramidates 12.
REACTION DE WITTIG-HORNER et TRANSFORMATION DES ALDEHYDES ET CETONES EN AMINES SUPERIEURES I. UN NOUVEAU REARRANGEMENT: IMINOPHOSPHONATES-PHOSPHORAMIDATES; MISE EN EVIDENCE ET ETUDE
Heymes, A.,Chekroun, I.
, p. 47 - 58 (2007/10/02)
The rearrangement in basic medium of A, (X,Y)P(O)-C(R)H-N=CH-, into B, (X,Y)P(O)-NH-C(R)=CH- is described for the first time.This transformation, sensitive to temperature, requires that R is hydrogen and that among X and Y one has to be an alkoxy group.For the rearrangement A-->B a mechanism is proposed which is analogous to the transformation of C, (X,Y)P(O)-C-NH-, into D, (X,Y)P(O)-N-C-H, described previously.
Process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine derivatives
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, (2008/06/13)
The present invention provides a process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine derivatives of the general formula: STR1 in which R1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, carboxyl, cyano or amino group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, the aminoethyl chain is in the 2- or 3-position, R2, R3 and R4, which are the same or different, are hydrogen atoms or heterocyclic or non-heterocyclic aromatic radicals, which are optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted.
Process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine derivatives
-
, (2008/06/13)
The present invention provides a multistep process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine intermediates of the general formula:- STR1 in which R1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, amino, cyano or carboxyl group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, R2 is a hydrogen atom, a linear or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, when the aminoethyl radical is in the two position and the radical R1 is in the 4- or 5-position, the above intermediates can be converted into 4,5,6,7-tetrahydrothieno[3,2-c]pyridine derivatives according to a procedure set forth in U.S. Pat. No. 4,127,580. When the aminoethyl radical is in the 3-position and the radical R1 is in the 4- or 5-position, the above intermediates can be converted into 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives according to a procedure set forth in U.S. Pat. No. 4,127,580. Both sets of tetrahydrothieno pyridine final products possess anti-inflammatory, vasodilator and blood platelet aggregation inhibition activity.
