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A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor

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Abstract

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.

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Authors and Affiliations

  1. Center for Process Research and Innovation, Dr. Reddy’s Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad, 500 046, Telangana, India

    Narasimha Rao Nevuluri, Rajesh Kumar Rapolu, Javed Iqbal, Bhaskar Kandagatla, Saikat Sen & Srinivas Oruganti

  2. Integrated Product Development Organization, Dr. Reddy’s Laboratories, Bachupally, Qutbullapur, Hyderabad, 500 090, Telangana, India

    Vilas H. Dahanukar

Authors
  1. Narasimha Rao Nevuluri
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  2. Rajesh Kumar Rapolu
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  3. Javed Iqbal
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  4. Bhaskar Kandagatla
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  5. Saikat Sen
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  6. Vilas H. Dahanukar
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  7. Srinivas Oruganti
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Corresponding author

Correspondence to Srinivas Oruganti.

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Nevuluri, N.R., Rapolu, R.K., Iqbal, J. et al. A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor. Monatsh Chem 148, 1477–1482 (2017). https://doi.org/10.1007/s00706-017-1920-1

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  • DOI: https://doi.org/10.1007/s00706-017-1920-1

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