Preparation method of valienamine from acarbose and/or...

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

Reexamination Certificate

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C536S123100, C514S054000, C514S061000, C564S462000

Reexamination Certificate

active

10519519

ABSTRACT:
The present invention provides a preparation method of valienamine from acarbose or acarbose derivatives using organic acid TFA (trifluoroacetic acid). By using the method of the present invention, valienamine, the core precursor of voglibose which is a strong retardant of α-glucosidase and which is used for the cure of diabetes, can be produced in large quantities by using selective hydrolysis from acarbose or acarbose derivatives using TFA.

REFERENCES:
patent: WO 2004000782 (2003-12-01), None
Tatsuta, Kuniaki, Mukai, Hiroshi and Takahashi, Masaaki, “Novel Synthesis of Natural Pseudo-aminosugars, (+)-Valienamine and (+)-Validamine”, The Journal of Antibiotics, vol. 53 No. 4, pp. 430-435, Apr. 2000.
Yoshikawa, Masayuki, Cha, Bae Cheon, Okaichi, Yoshihiko, Takinami, Yoshihiko, Yokokawa, Yoshihiro and Kitagawa, Isao, “Syntheses of Validamine, EPI-Validamine, and Valienamine, Three Optically Active Pseudo-Amino-Sugars, From D-Glucose”, Communications to the Editor, Chem. Pharm. Bull, vol. 36, pp. 4236-4239, 1988.

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