Enantiospecific Synthesis of (R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic Acid Using (S)-Serine as a Chiral Pool

Starting from (S)‐serine, a new method was developed for the synthesis of the β‐amino acid part of sitagliptin in ten steps and with an overall yield of 30%. The crucial step of the synthesis was the ring opening of N‐ and O‐protected (R)‐aziridin‐2‐methanol with (2,4,5‐trifluorophenyl)magnesium bro...

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Veröffentlicht in:	Helvetica chimica acta 2015-02, Vol.98 (2), p.260-266
Hauptverfasser:	Köse, Aytekin, Gündoğdu, Özlem, Aktaş, Derya, Fıstıkçı, Meryem, Altundaş, Ramazan, Seçen, Hasan, Kara, Yunus
Format:	Artikel
Sprache:	eng
Schlagworte:	(R)-3-amino-4- (S)-Serine 5-trifluorophenyl Aziridine Butanoic acid Butanoic acid, (R)‐3‐amino‐4‐(2,4,5‐trifluorophenyl) Sitagliptin
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