27471-36-9Relevant articles and documents
Preparation method of apixaban intermediate
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Paragraph 0039-0041, (2019/08/30)
The invention relates to a preparation method of an apixaban intermediate. The preparation method of the apixaban intermediate I comprises the following steps: p-chloroaniline, used as a raw material,and halide undergo an amidation and cyclization reaction under an alkaline condition to obtain 1-(4-chlorophenyl)piperidine-2-one, the 1-(4-chlorophenyl)piperidine-2-one and phosphorus pentachlorideundergo dichloro substitution, condensation-elimination and morpholine substitution to obtain the apixaban intermediate I. The method has the advantages of low cost, high reaction yield, and suitableness for industrial operation.
New synthetic routes for N-substituted 1,n-diamines. II. Synthesis of selectively N-substituted tetra- and pentamethylenediamines from ω-alkanoic acid derivatives
Ramírez, María A.,Corona, María V.,Ortiz, Gisela,Salerno, Alejandra,Perillo, Isabel A.,Blanco, María M.
supporting information; experimental part, p. 1466 - 1468 (2011/06/10)
A new approach for the synthesis of selectively N-substituted tetra- and pentamethylenediamines 1 (n = 4,5) is described. The method uses N-substituted ω-haloalkanamides 2 as precursors and involves the microwave-promoted conversion into ω-azidocarboxamides 3 and later the reduction of both azido and carboxamide groups with diborane.