A novel route for the synthesis of highly congested aryl-tethered 2-aminobenzylamines through ring transformation of 2-pyranones |
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Authors: | Farhanullah |
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Institution: | Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India |
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Abstract: | An innovative and efficient synthesis of highly congested 2-amino-3-aminomethyl-5-methylsulfanyl/sec-aminobiphenyl-4-carbonitriles 4 has been delineated through base catalyzed ring transformation of 6-aryl-4-methylsulfanyl/sec-amino-2H-pyran-2-one-3-carbonitriles 1 with Boc-protected 1,3-diamino-2-propanone 2, followed by TFA catalyzed hydrolysis of the intermediate 3-tert-butoxycarbonylaminomethyl-4-cyano-5-methylsulfanyl/sec-aminobiphenyl-2-yl]carbamic acid tert-butyl ester 3 in moderate yields as the TFA salts. |
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Keywords: | 2-Aminobenzylamine Ring transformation 2H-Pyran-2-one |
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