C07C271/18

Enantioselective synthesis of α-quaternary Mannich adducts by palladium-catalyzed allylic alkylation

This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): ##STR00001##
comprising treating a compound of formula (II): ##STR00002##
with a transition metal catalyst under alkylation conditions.

Enantioselective synthesis of α-quaternary Mannich adducts by palladium-catalyzed allylic alkylation

This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): ##STR00001##
comprising treating a compound of formula (II): ##STR00002##
with a transition metal catalyst under alkylation conditions.

Method for producing kakeromycin and derivatives thereof

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): ##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): ##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.

Method for producing kakeromycin and derivatives thereof

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): ##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): ##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.

Picolinamides as fungicides

This disclosure relates to picolinamides of Formula I and their use as fungicides. ##STR00001##

Picolinamides as fungicides

This disclosure relates to picolinamides of Formula I and their use as fungicides. ##STR00001##

CYCLIC PEPTIDES TARGETING ALPHA-4-BETA-7 INTEGRIN

There is described herein antagonists of α4β7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are various substituents; stereocentres 1*, 2* and 3* are each independently selected from R and S; n is 1, 2, 3, or 4 and where n is 2-4, Z is an amino terminus of an amino acid; —C═O— adjacent L is the carboxy terminus of an amino acid; and L along with Z and —C═O— is a peptide.

##STR00001##

CYCLIC PEPTIDES TARGETING ALPHA-4-BETA-7 INTEGRIN

There is described herein antagonists of α4β7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are various substituents; stereocentres 1*, 2* and 3* are each independently selected from R and S; n is 1, 2, 3, or 4 and where n is 2-4, Z is an amino terminus of an amino acid; —C═O— adjacent L is the carboxy terminus of an amino acid; and L along with Z and —C═O— is a peptide.

##STR00001##

Method for producing kakeromycin and derivatives thereof

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): ##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): ##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.

Method for producing kakeromycin and derivatives thereof

Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): ##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): ##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.