Development of the first and practical method for enantioselective synthesis of B-enriched p-borono-l-phenylalanine |
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| Authors: | Yoshihide Hattori Mitsunori Kirihata Tateaki Wakamiya |
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| Affiliation: | a Graduate School of Life and Environmental Sciences, Osaka Prefecture University, Sakai, Osaka 599-8231, Japan
b Faculty of Science and Technology, Kinki University, Higashi-osaka, Osaka 577-8502, Japan |
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| Abstract: | At present p-(10B)borono-l-phenylalanine (l-10Bpa) is used clinically as an excellent 10B carrier for BNCT; however, its enantioselective synthesis has not been reported yet. The present Letter describes the first and practical method for enantioselective synthesis of 10B-enriched l-Bpa using Z-l-Ser-OMe as the chiral synthon in good total yield and high optical purity. |
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| Keywords: | p-Boronophenylalanine BNCT Enantioselective synthesis 1,8-Diaminonaphtalene |
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