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ChemicalBook CAS DataBase List Avanafil
330784-47-9

Avanafil synthesis

1synthesis methods
Avanafil is a PDE5 inhibitor approved for erectile dysfunction by FDA on April 27, 2012 and by EMA on June 21, 2013. Avanafil is known by the trademark names Stendra and Spedra and was developed by Vivus Inc. Avanafil acts by inhibiting a specific phosphodiesterase type 5 enzyme which is found in various body tissues, but primarily in the corpus cavernosum penis, as well as the retina.
Synthetic Routes
  • ROUTE 1

    • 202112072063133975.jpg

    Sakamoto, Toshiaki; Koga, Yuichi; Hikota, Masataka; Matsuki, Kenji; Murakami, Michino; Kikkawa, Kohei; Fujishige, Kotomi; Kotera, Jun; Omori, Kenji; Morimoto, Hiroshi; Yamada, Koichiro. The discovery of avanafil for the treatment of erectile dysfunction: A novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor. Bioorganic & Medicinal Chemistry Letters. Volume 24. Issue 23. Pages 5460-5465. Journal; Online Computer File. (2014).

  • ROUTE 2

    • 202112073633956223.jpg

    Thirumalai, Rajan Srinivasan; Eswaraiah, Sajja; Satyanarayana, Komati. A process for the preparation of chloromethoxybenzylaminohydroxymethylpyrrolidinylpyrimidinylmethylpyrimidine carboxamide. Assignee MSN Laboratories Private Limited, India. IN 2013CH02915. (2015).

  • ROUTE 3

    • 202112079286192605.jpg

    Su, Xianbin; Guo, Jiasai; Jin, Kaijun; Dong, Haijun. Solid phase preparation method of avanafil applied in treatment of male erectile dysfunction. Assignee Nanjing University of Technology, Peop. Rep. China. CN 103435599. (2013).

  • ROUTE 4

    • 202112075492074289.jpg

    Chen, Lin; Gao, Heyong; Li, Wei. Avanafil intermediate, its preparing method and application. Assignee Angelisun (Chongqing) Pharmaceutical Co., Ltd., Peop. Rep. China. CN 104557877. (2015).

  • ROUTE 5

    • 202112072675029160.jpg

    Cui, Zhenwei; Zhang, Weiwei; Zhang, Fuqing. Preparation method of pharmaceutical compound Avanafil. Assignee Chongqing Aoshe Biochemical Co., Ltd., Peop. Rep. China. CN 109280050. (2019).

202112072063133975.jpg

Sakamoto, Toshiaki; Koga, Yuichi; Hikota, Masataka; Matsuki, Kenji; Murakami, Michino; Kikkawa, Kohei; Fujishige, Kotomi; Kotera, Jun; Omori, Kenji; Morimoto, Hiroshi; Yamada, Koichiro. The discovery of avanafil for the treatment of erectile dysfunction: A novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor. Bioorganic & Medicinal Chemistry Letters. Volume 24. Issue 23. Pages 5460-5465. Journal; Online Computer File. (2014).

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Yield:330784-47-9 99%

Reaction Conditions:

with dicyclohexyl-carbodiimide;1-hydroxy-1,2,3-benzotriazine-4(3H)-one in N,N-dimethyl-formamide at 0;Temperature;

Steps:

1 Preparation of avanafil

In the reaction flask, anhydrous DMF 3930 mL, compound 5 (393 g, 1.0 mol), 2-aminopyrimidine (163.5 g,1.5 mol), DCC (210 g, 1.02 mol) and 1-hydroxy-1,2,3-benzotriazine-4(3H)-one (166 g, 1.02 mol) at 0 ° CThe reaction was stirred, monitored until Compound 5 was completely reacted, filtered, and the filtrate was added to water, extracted with chloroform, washed with organic phase and dried.After the filtrate is too short, the silica gel layer is spin-dried to obtain crude avervavir, and the crude avervavir is purified by methanol to obtain pure avenue.The yield was 99.0% and the purity was 99.85%.

References:

CN109232542,2019,A Location in patent:Paragraph 0014; 0037-0038; 0048-0049; 0059-0060

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