6640-59-1Relevant articles and documents
A advantage Ralli sandbank intermediate and its preparation method and application
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, (2017/08/25)
The present invention relates to a linagliptin intermediate, a preparation method and applications thereof, wherein the linagliptin intermediate has the structure represented by general formulas (II) and (IV), and X is halogen. According to the present invention, the compound of the present invention is the solid and has characteristics of low production cost, easy purification and easy storage, linagliptin can be efficiently prepared, and the method is suitable for industrial scale production.
Mechanism of selective formation of 2-amino-substituted 1,4-benzodiazepin-4-oxides and 2-aminomethyl substituted quinazolin-3-oxides from chloromethyl quinazolin-N-oxides indications from perturbation theory
Lessel
, p. 77 - 84 (2007/10/02)
The o-amino-acetophenone and -benzophenone oximes 1a-c react with chloroacetyl chloride giving the 2-chloromethyl-quinazoline-3-oxides 6a-c. The mechanism is explained using the perturbation theory. With ammonia and N-prim. aliphatic amines, compounds 6a-c yield 1,4-benzodiazepines 16 and 17 as ring-enlarged products, with aromatic and with N-sec. aliphatic amines, quinazoline derivatives 10-13 are formed. The constitution of the heterocycles is proved by nmr spectroscopic methods. Selective formation of the heterocyclic products is explained with the relative thermodynamic stability of the corresponding 2-adducts 14.