A novel convergent method for the synthesis of α-acyl-γ-hydroxylactams and its application in the total synthesis of PI-090 and 091

Uchiro, Hiromi; Shionozaki, Nobuhiro; Kobayakawa, Yu; Nakagawa, Hiroko; Makino, Kimiko

A novel convergent method for the synthesis of α-acyl-γ-hydroxylactams and its application in the total synthesis of PI-090 and 091

2012

Uchiro, Hiromi | Shionozaki, Nobuhiro | Kobayakawa, Yu | Nakagawa, Hiroko | Makino, Kimiko

A novel convergent method for the synthesis of α-acyl-γ-hydroxylactams utilizing the aldol reaction of N-Boc-protected γ-methoxylactams was developed. As the first application of this method for the synthesis of biologically active natural products, the total synthesis of platelet aggregation inhibitors PI-090 and PI-091 were also investigated and successfully achieved.

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