The present invention relates to a process for preparing tc-DNA nucleoside precursors, the resulting tc-DNA nucleosides, and oligonucleotides comprising such tc-DNA nucleosides. In an embodiment of the invention, the process includes use of a carbene precursor.

The present invention relates to a process for preparing tc-DNA nucleoside precursors, the resulting tc-DNA nucleosides, and oligonucleotides comprising such tc-DNA nucleosides. In an embodiment of the invention, the process includes use of a carbene precursor.

Disclosed herein is the catalyst-controlled site-selective activation of - and -methylene CH bonds of free carboxylic acids which heretofore was unknown and has remained a tremendous challenge. Described herein in the enablement of such chemical reactivity with ubiquitous dicarboxylic acids which possess inert, methylene-rich backbones and dual functional groups which opened up pathways for the construction of complex molecular scaffolds for organic synthesis. Herein we show that with a pair of palladium catalysts, it is possible to perform highly site-selective monolactonization reactions with a wide range of dicarboxylic acids, generating topologically diverse and synthetically useful - and -lactones via site-selective - or -methylene CH activation. The remaining carboxyl group serves as a versatile linchpin for further synthetic applications as demonstrated by the total synthesis of two natural products, myrotheciumone A and pedi cellosine, from abundant dicarboxylic acids.

Disclosed herein is the catalyst-controlled site-selective activation of - and -methylene CH bonds of free carboxylic acids which heretofore was unknown and has remained a tremendous challenge. Described herein in the enablement of such chemical reactivity with ubiquitous dicarboxylic acids which possess inert, methylene-rich backbones and dual functional groups which opened up pathways for the construction of complex molecular scaffolds for organic synthesis. Herein we show that with a pair of palladium catalysts, it is possible to perform highly site-selective monolactonization reactions with a wide range of dicarboxylic acids, generating topologically diverse and synthetically useful - and -lactones via site-selective - or -methylene CH activation. The remaining carboxyl group serves as a versatile linchpin for further synthetic applications as demonstrated by the total synthesis of two natural products, myrotheciumone A and pedi cellosine, from abundant dicarboxylic acids.

Described herein are N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl) carbamoyl)-4,5,6,7-tetrahydrobenzofuran-2-sulfonamide derivatives and related compounds of formula (I) wherein R1 is formulae (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX) and R2 is formulae (X) or (XI) as NLRP3 (pyrin domain-containing protein 3) modulators for the treatment of e.g. metabolic diseases (e.g. type 2 diabetes or obesity), liver diseases (e.g. NAFLD or cirrhosis), lung diseases (e.g. asthma or CORD), central nervous system diseases (e.g. Alzheimer's disease or multiple sclerosis), inflammatory or autoimmune diseases (e.g. rheumatoid arthritis or psoriasis), cardiovascular diseases (e.g. atherosclerosis or stroke). The present description discloses the synthesis and characterization of exemplary compounds as well as pharmacological data thereof. An exemplary compound is e.g. N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl) carbamoyl)-4-hydroxy-4-methyl-4,5,6,7-tetrahydrobenzofuran-2-sulfonamide (Example 1; compound (5)). ##STR00001## ##STR00002##

Described herein are N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl) carbamoyl)-4,5,6,7-tetrahydrobenzofuran-2-sulfonamide derivatives and related compounds of formula (I) wherein R1 is formulae (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX) and R2 is formulae (X) or (XI) as NLRP3 (pyrin domain-containing protein 3) modulators for the treatment of e.g. metabolic diseases (e.g. type 2 diabetes or obesity), liver diseases (e.g. NAFLD or cirrhosis), lung diseases (e.g. asthma or CORD), central nervous system diseases (e.g. Alzheimer's disease or multiple sclerosis), inflammatory or autoimmune diseases (e.g. rheumatoid arthritis or psoriasis), cardiovascular diseases (e.g. atherosclerosis or stroke). The present description discloses the synthesis and characterization of exemplary compounds as well as pharmacological data thereof. An exemplary compound is e.g. N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl) carbamoyl)-4-hydroxy-4-methyl-4,5,6,7-tetrahydrobenzofuran-2-sulfonamide (Example 1; compound (5)). ##STR00001## ##STR00002##

Methods for the synthesis of a tricyclic-prostaglandin D.sub.2 metabolite methyl ester or a pharmaceutically acceptable salt thereof.

Methods for the synthesis of a tricyclic-prostaglandin D.sub.2 metabolite methyl ester or a pharmaceutically acceptable salt thereof.