Abstract: Provided is a method of producing an antibody-drug conjugate represented by Formula I in the formula, Ab is an antibody or an antigen-binding fragment thereof, D is eribulin, m is an integer of 1 to 10, and p is an integer of 1 to 8, the method comprising: a step 1 of obtaining a compound represented by Formula (B) by reaction of eribulin or a salt thereof with a compound represented by Formula (A), in the formula, m is an integer of 1 to 10 and X is a phenoxy group or a nitrophenoxy group, and in the formula, n is an integer of 1 to 10, and a step 2 of obtaining the antibody-drug conjugate represented by Formula (I) by reaction of the compound represented by Formula (B) with Ab.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.

Abstract: This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12.

Abstract: A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.

Abstract: A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or —CH(Y)— where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.

Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).

Abstract: The invention provides crystals of dihydrochloride monohydrate of the compound of the following formula having an A? production inhibiting effect which crystals are characterized by exhibiting a diffraction peak at an angle of diffraction (2?±0.2°) of 10.9° in powder X-ray diffractometry. Further, the invention also provides the compound in the form of various salts, crystal forms and amorphous forms which are suitable for the development of drugs.

Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).

Abstract: The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 ?, a process for producing them, and a powdery charged preparation for injection containing them.

Abstract: The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 ?, a process for producing them, and a powdery charged preparation for injection containing them.

Abstract: The object of the invention is to provide a process for efficient, inexpensive and stereoselective production of (2S,4S)-2-[[(3R)-pyrrolidin-3-yl-(R)-hydroxylmethyl]pyrrolidin-4-thiol dihydrochloride useful as an intermediate in production of novel carbapenem, and the intermediate is produced via a novel crystallizable intermediate (2S,4R)—N-t-butoxycarbonyl-2-[[(3R)—N-t-butoxycarbonyl pyrrolidin-3-yl-(R)-hydroxylmethyl]-4-hydroxypyrrolidine from a (2S,4R)-4-alkylsilyloxy-N-t-butoxycarbonylpyridine-2-carbaldehyde derivative by aldol reaction using an asymmetric assistant such as amino-alcohol.

Abstract: A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak—E means the alkali earth metal; and B means the inorganic acid, respectively.