Catalyzed process of making C-5-substituted heterocyclic...

Details Catalyzed process of making C-5-substituted heterocyclic... Catalyzed process of making C-5-substituted heterocyclic...

2006-11-01

2009-06-02

Saeed, Kamal A (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S225000

Reexamination Certificate

active

07541474

ABSTRACT:
The invention provides a process for preparing 11 β-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base:where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

REFERENCES:
patent: WO 2005/116002 (2005-12-01), None
patent: WO 2007/061600 (2007-05-01), None
Vippagunta et al., Crystalline solids, 2001, Advanced Drug Delivery Reviews, 48, pp. 3 and 18.
Lee, et al., “Palladium-Catalyzed α-Arylation of Esters and Protected Amino Acids,”J. Am. Chem. Soc., vol. 123, pp. 8410-8411, 2001.
Splelvogel, et al., “Nickel-BINAP Catalyzed Enantioselective α-Arylation of α-Substituted γ-Butyrolactones,”J. Am. Chem. Soc., vol. 124, pp. 3500-3501, 2002.
Hamada, et al., “An Improved Catalyst for the Asymmetric Arylation of Ketone Enolates,”J. Am. Chem. Soc., vol. 124, No. 7, pp. 1261-1268, 2002.
Kawatsura, et al., “Simple, Highly Active Palladium Catalysts for Ketone and Malonate Arylation: Dissecting the Importance of Chelation and Steric Hindrance,”J. Am. Chem. Soc., vol. 121, pp. 1473-1478, 1999.
Stauffer, et al., Palladium-Catalyzed Arylation of Ethyl Cyanoacetate, Fluorescence Reasonance Energy Transfer as a Tool for Reaction Discovery,J. Am. Chem. Soc., vol. 123, pp. 4641-4642, 2001.
Metzger et al., “Comportement et reactivite d'heterocycloammoniums dans la synthese des colorants cyanines et carbocyanines,”Bulletin de la Societe Chimique de France, 1967, pp. 30-40 (XP009081230).
Patnaik et al., “Preparation of Some 5-Substituted 2-arylimino-4-thiazolidines,”J. Indian Chem. Soc., vol. 34, No. 11, 1957, pp. 814-816, (XP009081229).

Affiliated with

Also associated with

Rating

Catalyzed process of making C-5-substituted heterocyclic... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Catalyzed process of making C-5-substituted heterocyclic..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Catalyzed process of making C-5-substituted heterocyclic... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4116808