A three step continuous flow synthesis of the biaryl unit of the HIV protease inhibitor Atazanavir.

A three step continuous flow synthesis of the biaryl unit of the HIV protease inhibitor Atazanavir.

Vechia, Luciana Dalla; Reichart, Benedikt; Glasnov, Toma; Miranda, Leandro S. M.; Kappe, C. Oliver; Souza, Rodrigo O. M. A. de

Abstract:

Continuous flow technology has attracted the attention of the organic chemistry community in the last decade, both as an enabling tool to enhance organic synthesis and as a manufacturing method. The continuous flow synthesis of active pharmaceutical ingredients (APIs), which typically involve a significant number of synthetic steps, therefore clearly is a rather complex operation. Atazanavir is one of the most prescribed protease inhibitors in Brazil (and worldwide) and thus a sufficient and cost effective supply to Atazanavir is of prime importance. The retrosynthetic analysis for the Atazanavir (1) molecule is shown in Figure 1 and reveals an assembly three different building blocks.

Continuous flow technology has attracted the attention of the organic chemistry community in the last decade, both as an enabling tool to enhance organic synthesis and as a manufacturing method. The continuous flow synthesis of active pharmaceutical ingredients (APIs), which typically involve a significant number of synthetic steps, therefore clearly is a rather complex operation. Atazanavir is one of the most prescribed protease inhibitors in Brazil (and worldwide) and thus a sufficient and cost effective supply to Atazanavir is of prime importance. The retrosynthetic analysis for the Atazanavir (1) molecule is shown in Figure 1 and reveals an assembly three different building blocks.

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DOI: 10.5151/chempro-15bmos-BMOS2013_2013917165936

Referências bibliográficas

• [1] 1 Noël, T.; Buchwald, S. L. Chem. Soc. Rev. 2011, 5010.
• [2] 2 Xu, Z. et al. Org. Process Res. Dev. 2002, 323.

Como citar:

Vechia, Luciana Dalla; Reichart, Benedikt; Glasnov, Toma; Miranda, Leandro S. M.; Kappe, C. Oliver; Souza, Rodrigo O. M. A. de; "A three step continuous flow synthesis of the biaryl unit of the HIV protease inhibitor Atazanavir.", p-286-286. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 2, Dezembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-15bmos-BMOS2013_2013917165936