- Concise Synthesis of (±)-Clopidogrel via Carboxylation of Benzylamine with CO2
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A concise and efficient synthesis of (±)-clopidogrel, an antithrombotic agent, is achieved by inserting CO2 at the benzylic position as the key reaction without using any toxic transition metals. The overall yield of the synthetic process is 38% and the salient features include operationally simple process chemistry and fewer steps.
- Venkataramasubramanian,Sudalai, Arumugam
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supporting information
p. 2099 - 2105
(2015/09/01)
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- One pot synthesis of 5-(substituted aryl) methyl-4,5,6,7-tetrahydrothieno [3,2-c] pyridine using chloromethyl methyl ether
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Ticlopidine and its analogues were prepared by one pot synthesis without isolating the intermediates. This sequential one pot synthesis avoided a lengthy separation process, workup and purification of the intermediate compounds and thus could save the time and resources and increased the yield.
- Rege, Chandana M.,Gadre,Bhalekar, Satish M.
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p. 197 - 198
(2013/09/23)
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- N-2-chlorobenzyl-2-oxo and N-2-chlorobenzyl-2,2-dioxo-1,2,3-oxathiazolidine derivatives, their preparation and synthesis of thieno[3,2-c]pyridine derivatives therefrom
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Compounds of the formula: STR1 wherein: A is oxo or dioxo; R1, R2 and R3 are independently hydrogen or lower alkyl of one to six carbon atoms; R4, R5, R6 and R7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo; are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
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- Process for the preparation of N-(2-chlorobenzyl)-2-(2-thienyl) ethylamine
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In the process according to the invention 2-thiophene acetonitrile is reacted with 2-chlorobenzylamine and hydrogen in the presence of a hydrogenation catalyst. The product obtained is a chemical intermediate useful in the pharmaceutical industry.
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- PO-Activated Olefination and Conversion of Aldehydes and Ketones to Higher Amines; II. Synthesis of Arylethylamines
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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.
- Heymes, A.,Chekroun, I.
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p. 245 - 249
(2007/10/02)
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- REACTION DE WITTIG-HORNER et TRANSFORMATION DES ALDEHYDES ET CETONES EN AMINES SUPERIEURES I. UN NOUVEAU REARRANGEMENT: IMINOPHOSPHONATES-PHOSPHORAMIDATES; MISE EN EVIDENCE ET ETUDE
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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.
- Heymes, A.,Chekroun, I.
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- Process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine derivatives
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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.
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