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Diastereoselective synthesis of Pro-Phe phosphinyl dipeptide isosteres |
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| Authors: | Takehiro Yamagishi Atsushi Kinbara Noriko Okubo Shunpei Sato Haruhiko Fukaya |
| Affiliation: | 1. School of Pharmacy, Ohu University, 31-1 Tomita-machi, Misumidou, Kooriyama, Fukushima 963-8611, Japan;2. School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan |
| Abstract: | The diastereoselective synthesis of Pro-Phe phosphinyl dipeptide isosteres in protected form was achieved by starting from optically active 1,1-diethoxyethyl(aminomethyl)phosphinate. Our methodology involves diastereoselective α-alkylation and β′-alkylation of phosphinate derivatives with an asymmetric center at the phosphorus atom. |
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