137864-22-3Relevant articles and documents
Synthesis of 5-Substituted 1 H-Tetrazoles from Nitriles by Continuous Flow: Application to the Synthesis of Valsartan
Carpentier, Florian,Felpin, Fran?ois-Xavier,Zammattio, Fran?oise,Le Grognec, Erwan
, p. 752 - 761 (2020/03/13)
An efficient continuous flow process for the synthesis of 5-substituted 1H-tetrazoles is described. The process involves the reaction between a polymer-supported triorganotin azide and organic nitriles. The polymer-supported organotin azide, which is in situ generated with a polystyrene-supported triorganotin alkoxide and trimethylsilylazide, is immobilized in a packed bed reactor. This approach is simple, fast (it takes from 7.5 to 15 min), and guarantees a low concentration of tin residues in the products (5 ppm). The process was developed to aryl-, heteroaryl-, and also alkylnitriles and was applied for the synthesis of valsartan, an angiotensin II receptor antagonist.
PROCESS FOR PREPARATION OF VALSARTAN INTERMEDIATE
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, (2009/11/29)
The present invention provides a process for preparation of a key intermediate of valsartan in a pure form and use of this intermediate for the preparation of valsartan or a pharmaceutically acceptable salt in pure form.
Process for the preparation of valsartan and its intermediates
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Page/Page column 7, (2010/11/25)
The present invention relates to an improved process for the preparation of valsartan and its intermediates in substantially pure enantiomeric form. In particular, the present invention provides a process for preparing benzyl valsartan intermediate substantially free of organotin impurities. The valsartan produced from such benzyl valsartan intermediate requires significantly lower catalyst loading and has superior purity.