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.

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.

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.

This invention includes ionizable compounds, and compositions and methods of use thereof. The ionizable compounds can be used for making nanoparticle compositions for use in biopharmaceuticals and therapeutics. More particularly, this invention relates to compounds, compositions and methods for providing nanoparticles to encapsulate active agents, such as nucleic acid agents, and to deliver and distribute the active agents to cells, tissues, organs, and subjects.

This invention includes ionizable compounds, and compositions and methods of use thereof. The ionizable compounds can be used for making nanoparticle compositions for use in biopharmaceuticals and therapeutics. More particularly, this invention relates to compounds, compositions and methods for providing nanoparticles to encapsulate active agents, such as nucleic acid agents, and to deliver and distribute the active agents to cells, tissues, organs, and subjects.

The present invention relates to the field of synthesis of drug intermediates, in particular to the field of synthesis of key intermediates for preparing the anti-rheumatoid arthritis drug tofacitinib. Specifically, provided are a 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine compound, a synthetic method thereof, and the use thereof in the preparation of a key intermediate cis-1-benzyl-3-methylamino-4-methylpiperidine of tofacitinib.

The present invention relates to the field of synthesis of drug intermediates, in particular to the field of synthesis of key intermediates for preparing the anti-rheumatoid arthritis drug tofacitinib. Specifically, provided are a 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine compound, a synthetic method thereof, and the use thereof in the preparation of a key intermediate cis-1-benzyl-3-methylamino-4-methylpiperidine of tofacitinib.

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a dimethyl-nonatetraenyl-trimethyl-cyclohexyl structure useful as therapeutics for the treatment of subjects suffering from disorders characterized by abnormal proliferation and/or abnormal differentiation of cells, in particular of cells of which the growth and differentiation is sensitive to the actions of retinoids.

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.

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.