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: The present invention relates to a composition comprising a plurality of sodium salts represented by the formula (I): wherein, m1, n1, m2 and n2 respectively and independently represent a positive number between 0 and 2, provided that m1+n1=2, m2+n2=2, 0<m1+m2<4 and 0<n1+n2<4, and a method for producing the same, and a method for inhibiting the decomposition of a sodium salt represented by general formula (IV): comprising: having the sodium salt represented by general formula (IV) in the presence of the sodium salts represented by formula (I), and according to the present invention the stability over time of the sodium salt represented by general formula (IV) is improved.

Abstract: Disclosed are a sodium salt represented by the average formula (I) below, and a method for producing such a sodium salt. (In the formula, m1, n1, m2 and n2 independently represent 0 or a positive number not greater than 2, while satisfying m1+n1=2, m2+n2=2, 0<m1+m2<4 and 0<n1+n2<4.) Also disclosed is a decomposition suppression method which makes a sodium salt represented by average formula (I) coexist with a sodium salt represented by the general formula (IV) below. This method enables improvement of long-term stability of a sodium salt represented by general formula (IV).

Abstract: Discloses is a process for producing ?-D-glucopyranose, 3-O-decyl-2-deoxy-6-O-[2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[(11Z)-1-oxo-11-octadecenyl]amino]-4-O-phosphono-?-D-glucopyranosyl]-2-[(1,3-dioxotetradecyl)amino]- or 1-(dihydrogen phosphate) tetrasodium salt which is useful as an active ingredient of a pharmaceutical or an intermediate for the synthesis thereof, which is environment-friendly and excellent in safety, operationality and reproducibility. A process for producing a compound represented by the formula (I) comprising the steps of reacting a compound represented by the formula (VIII) with a palladium catalyst in the presence of a nucleopholic agent and treating the product with a sodium source.

Abstract: The present invention relates to a sodium salt represented by average formula (I): (wherein, m1, n1, m2 and n2 respectively and independently represent a positive number of 0 0r 2 or less, provided that m1+n1=2, m2+n2=2, 0<m1+m2<4 and 0<n1+n2<4), a method for producing the same, and a method for inhibiting decomposition of a sodium salt represented by general formula (IV): [CHEMICAL 4] comprising: having the sodium salt represented by general formula (IV) in the presence of the sodium salt represented by average formula (I), and according to the present invention the stability over time of the sodium salt represented by general formula (IV) is improved.

Abstract: To provide a novel, industrially superior process for producing a 1,4-substituted cyclic amine compound which is useful as a pharmaceutical, and an intermediate for the process. That is, a process for producing an indole compound (I), which comprises reducing a 1,4-subsutituted 2-nitrophenyl compound (VII) to give a 1,4-substituted 2-aminophenyl compound (V); reacting the compound (V) with an N-substituted 4-piperidone compound (VI) to give a 1,4-substituted 2-piperidylaminophenyl compound (IV); cyclizing the compound (IV) to give a 2-oxoindoline compound (III); halogenating the compound (III) to give a 2-halogenated indole compound (II); reducing the compound (II); and if necessary subjecting the resulting compound to alcoholysis or aminolysis. wherein each of R1 and R2 represents a substituent; X represents a halogen atom; and n is a numerical subscript.