C07C62/38

Pd(II)-catalyzed enantioselective C—H arylation of free carboxylic acids

The invention includes procedures for stereoselective β-acylation of carboxylic acids having a β-carbon atom. For example, stereoselective acylation procedures include the following reactions: (I) ##STR00001##

Pd(II)-catalyzed enantioselective C—H arylation of free carboxylic acids

The invention includes procedures for stereoselective β-acylation of carboxylic acids having a β-carbon atom. For example, stereoselective acylation procedures include the following reactions: (I) ##STR00001##

Anti-fungal compounds

The present disclosure provides compounds of the formula (I), (II), (III), wherein the variables are as defined herein for use in the treatment of fungal infections. In some embodiments, the fungal infection is an infection of Cryptococcus neojormans fungus. Also provided herein are compositions comprising a compound of formula I, II, or III and a second anti-fungal agent. ##STR00001##

Anti-fungal compounds

The present disclosure provides compounds of the formula (I), (II), (III), wherein the variables are as defined herein for use in the treatment of fungal infections. In some embodiments, the fungal infection is an infection of Cryptococcus neojormans fungus. Also provided herein are compositions comprising a compound of formula I, II, or III and a second anti-fungal agent. ##STR00001##

PD(II)-CATALYZED ENANTIOSELECTIVE C-H ARYLATION OF FREE CARBOXYLIC ACIDS
20210087131 · 2021-03-25 ·

The invention includes procedures for stereoselective -acylation of carboxylic acids having a -carbon atom. For example, stereoselective acylation procedures include the following reactions: (I)

##STR00001##

PD(II)-CATALYZED ENANTIOSELECTIVE C-H ARYLATION OF FREE CARBOXYLIC ACIDS
20210087131 · 2021-03-25 ·

The invention includes procedures for stereoselective -acylation of carboxylic acids having a -carbon atom. For example, stereoselective acylation procedures include the following reactions: (I)

##STR00001##

Compositions and methods for inhibiting influenza RNA polymerase PA endonuclease

There are provided inter alia metalloenzyme inhibitors, such as inhibitors of influenza A RNA dependent RNA polymerase PA subunit endonuclease, and methods of synthesis and use of the same.

Compositions and methods for inhibiting influenza RNA polymerase PA endonuclease

There are provided inter alia metalloenzyme inhibitors, such as inhibitors of influenza A RNA dependent RNA polymerase PA subunit endonuclease, and methods of synthesis and use of the same.

Complex and structurally diverse compounds

The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.

Complex and structurally diverse compounds

The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.