Patent classifications
C07D309/32
COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION OF COMPOUND IN PREPARATION OF BICYCLOPYRONE INTERMEDIATE
Through an intermediate I (a compound having the structural formula as shown in the formula Ia and/or the formula Ib), or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a tautomer Ic of Ib, a bicyclopyrone intermediate II with a high yield can be prepared. Two compounds are docked first under the action of a base to produce an intermediate I, and then the intermediate I is subjected to intramolecular ring closure by an ammonium salt, which can increase the yield of the bicyclopyrone intermediate (II), reduce side reactions, and reduce problems that a reaction of raw materials is easily incomplete due to intramolecular ring closure directly through an ammonium salt. A one-pot method includes producing an intermediate I under the action of a base and then performing a ring-closure reaction to produce a bicyclopyrone intermediate (II) that reduces side reactions, and further increases the yield.
COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION OF COMPOUND IN PREPARATION OF BICYCLOPYRONE INTERMEDIATE
Through an intermediate I (a compound having the structural formula as shown in the formula Ia and/or the formula Ib), or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a tautomer Ic of Ib, a bicyclopyrone intermediate II with a high yield can be prepared. Two compounds are docked first under the action of a base to produce an intermediate I, and then the intermediate I is subjected to intramolecular ring closure by an ammonium salt, which can increase the yield of the bicyclopyrone intermediate (II), reduce side reactions, and reduce problems that a reaction of raw materials is easily incomplete due to intramolecular ring closure directly through an ammonium salt. A one-pot method includes producing an intermediate I under the action of a base and then performing a ring-closure reaction to produce a bicyclopyrone intermediate (II) that reduces side reactions, and further increases the yield.
Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols
The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic -quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.
Methods for enantioselective allylic alkylation of esters, lactones, and lactams with unactivated allylic alcohols
The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic -quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds that are useful for treating or preventing cancer.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds that are useful for treating or preventing cancer.
TARGETED CYTOTOXIC RATJADONE DERIVATIVES AND CONJUGATES THEREOF
The present invention is directed to novel natural product-derived ratjadone-based compounds useful as payloads (or toxins) in drug-conjugates constructs with cell target binding moieties (CTBM) and payload-linker compounds useful in connection with drug conjugates. The present invention further relates to new ratjadone compositions including the aforementioned payloads, payload-linkers and drug conjugates, and methods for using these payloads, payload-linkers and drug conjugates, to treat pathological conditions including cancer, inflammatory and infectious diseases.
TARGETED CYTOTOXIC RATJADONE DERIVATIVES AND CONJUGATES THEREOF
The present invention is directed to novel natural product-derived ratjadone-based compounds useful as payloads (or toxins) in drug-conjugates constructs with cell target binding moieties (CTBM) and payload-linker compounds useful in connection with drug conjugates. The present invention further relates to new ratjadone compositions including the aforementioned payloads, payload-linkers and drug conjugates, and methods for using these payloads, payload-linkers and drug conjugates, to treat pathological conditions including cancer, inflammatory and infectious diseases.
BIOSYNTHETIC PATHWAYS AND PRODUCTS
This disclosure describes biosynthesized compounds including anhydromevalonolactone and -methyl--valerolactone. This disclosure further describes biosynthetic methods for making these compounds. In some embodiments, the biosynthetic methods can include a combination of biosynthesis and chemical steps to produce -methyl--valerolactone. Finally, this disclosure described recombinant cells useful for the biosynthesis of these compounds.
BIOSYNTHETIC PATHWAYS AND PRODUCTS
This disclosure describes biosynthesized compounds including anhydromevalonolactone and -methyl--valerolactone. This disclosure further describes biosynthetic methods for making these compounds. In some embodiments, the biosynthetic methods can include a combination of biosynthesis and chemical steps to produce -methyl--valerolactone. Finally, this disclosure described recombinant cells useful for the biosynthesis of these compounds.