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2001 tetrazole derivatives tetrazole derivatives R 0310 13 - 133 Fast Microwave-Assisted Preparation of Aryl and Vinyl Nitriles and the Corresponding Tetrazoles from Organo-Halides. Palladium- catalyzed reaction of aryl and vinyl bromides (I) with Zn(CN) 2 proceeds in 2–3 minutes under microwave irradiation (60W) providing the aryl or vinyl nitriles (III) in yields comparable to thermal reaction. Additionally, conversion of these nitriles to the corresponding tetrazole derivatives (IV) is efficiently sped up under microwave irradiation (20W). This tetrazole formation can be carried out in a one-pot procedure starting from aryl bromide, as demonstrated for phenyltetrazole (VI) as well as for compound (VII), a potent HIV-1 protease inhibitor. — (ALTERMAN, MATHIAS; HALLBERG, ANDERS; J. Org. Chem. 65 (2000) 23, 7984-7989; Dep. Org. Pharm. Chem., Biomed. Cent., Uppsala Univ., S-751 23 Uppsala, Swed.; EN) 1

ChemInform Abstract: Fast Microwave-Assisted Preparation of Aryl and Vinyl Nitriles and the Corresponding Tetrazoles from Organo-Halides

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Page 1: ChemInform Abstract: Fast Microwave-Assisted Preparation of Aryl and Vinyl Nitriles and the Corresponding Tetrazoles from Organo-Halides

2001 tetrazole derivatives

tetrazole derivativesR 0310

13 - 133Fast Microwave-Assisted Preparation of Aryl and Vinyl Nitriles andthe Corresponding Tetrazoles from Organo-Halides. — Palladium-catalyzed reaction of aryl and vinyl bromides (I) with Zn(CN)2 proceeds in 2–3minutes under microwave irradiation (60W) providing the aryl or vinyl nitriles(III) in yields comparable to thermal reaction. Additionally, conversion of thesenitriles to the corresponding tetrazole derivatives (IV) is efficiently sped upunder microwave irradiation (20W). This tetrazole formation can be carriedout in a one-pot procedure starting from aryl bromide, as demonstrated forphenyltetrazole (VI) as well as for compound (VII), a potent HIV-1 proteaseinhibitor. — (ALTERMAN, MATHIAS; HALLBERG, ANDERS; J. Org.Chem. 65 (2000) 23, 7984-7989; Dep. Org. Pharm. Chem., Biomed. Cent.,Uppsala Univ., S-751 23 Uppsala, Swed.; EN)

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