503614-56-0Relevant articles and documents
Preparation method of apixaban and intermediates thereof
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Paragraph 0082-0097, (2018/05/16)
The invention discloses a preparation method of apixaban and intermediates thereof. The invention provides a preparation method of an apixaban intermediate I. The preparation method of the apixaban intermediate I comprises the step of performing nucleophilic substitution reaction on an apixaban intermediate II and p-fluoronitrobenzene in an organic solvent in the presence of an alkali to obtain the apixaban intermediate I. The preparation method has short steps, simple and safe operation, simple post-treatment steps, environmental friendliness and high total yield, and the obtained product hashigh purity, low production cost and high atomic utilization, and is suitable for industrial production. The formula is shown in the description.
LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
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, (2017/04/28)
The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor
Nevuluri, Narasimha Rao,Rapolu, Rajesh Kumar,Iqbal, Javed,Kandagatla, Bhaskar,Sen, Saikat,Dahanukar, Vilas H.,Oruganti, Srinivas
, p. 1477 - 1482 (2017/07/18)
A convergent synthesis of the anti-coagulant drug apixaban has been efficiently demonstrated on a multi-gram scale. The synthetic route is noteworthy for its brevity and fact that it completely avoids the use of morpholine, a toxic and flammable reagent, in constructing the 5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one core present in apixaban. Graphical abstract: [Figure not available: see fulltext.].