Concepedia

Development of a Scalable and Safe Procedure for the Production of (3R)-3-(2,3-Dihydro-1-benzofuran-5-yl)-1,2,3,4-tetrahydro-9H-pyrrolo[3,4-b]- quinolin-9-one, an Intermediate in the Synthesis of PDE-V Inhibitors RWJ387273 (R301249) and RWJ444772 (R290629)

Bert Willemsens, Ivan Vervest, Dominic Ormerod, Wim Aelterman, Christine Fannes, Narda Mertens, István E. Markó, Sébastien Lemaire

Organic Process Research & Development · 2006 · 12 citations · 1 references

DOI

Concepts

PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoverySynthetic Medicinal ChemistryEnzyme InhibitionSafer Chemical SynthesisMedicinal Chemistry ApplicationsQuinoline ChemistryQuinoline Synthesis

Abstract

A scalable and safe process for the oxidative rearrangement of β-carboline to quinolone derivatives, intermediates in the synthesis of PDE-V inhibitors RWJ387273 (R301249) and RWJ444772 (R290629), has been developed.

References

1

An Efficient Process for Synthesis of 3-(R)-3-(2,3-Dihydrobenzofuran-5-yl)- 1,2,3,4-tetrahydropyrrolo[3,4-b]quinolin-9-one

Xun Li, Shawn Branum, Ronald K. Russell et al. · Organic Process Research & Development · 2005 · 16 citations

Pharmacy, Medicinal Chemistry, Pharmacology +13

Development of a Scalable and Safe Procedure for the Production of (3<i>R</i>)-3-(2,3-Dihydro-1-benzofuran-5-yl)-1,2,3,4-tetrahydro-9<i>H</i>-pyrrolo[3,4-<i>b</i>]- quinolin-9-one, an Intermediate in the Synthesis of PDE-V Inhibitors RWJ387273 (R301249) and RWJ444772 (R290629)

Concepts

Abstract

References