A concise synthesis of (S)-N-ethoxycarbonyl-alpha-methylvaline |
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Authors: | Kuethe Jeffrey T Gauthier Donald R Beutner Gregory L Yasuda Nobuyoshi |
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Institution: | Department of Process Research, Merck & Co. Inc., Rahway, NJ 07065, USA. jeffrey_kuethe@merck.com |
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Abstract: | A practical and efficient protocol for the three-step synthesis of (S)-N-ethoxycarbonyl-alpha-methylvaline 3 is described which utilizes readily available commercial starting materials. The key transformations involve resolution-crystallization of tartrate salt 6 followed by a one-pot procedure for the preparation of 3 which is isolated as the dicyclohexylamine salt in 45% overall yield and in 91-95% ee. |
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