C07D207/448

METHODS OF PREPARING CYTOTOXIC BENZODIAZEPINE DERIVATIVES
20200172481 · 2020-06-04 ·

The invention provides novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

Cysteine engineered fibronectin type III domain binding molecules

Cysteine engineered monospecific and bispecific EGFR and/or c-Met FN3 domain containing molecules comprising one or more free cysteine amino acids are prepared by mutagenizing a nucleic acid sequence of a parent molecule and replacing one or more amino acid residues by cysteine to encode the cysteine engineered FN3 domain containing monospecific or bispecific molecules; expressing the cysteine engineered FN3 domain containing molecules; and recovering the cysteine engineered FN3 domain containing molecule. Isolated cysteine engineered monospecific or bispecific FN3 domain containing molecules may be covalently attached to a detection label or a drug moiety and used therapeutically.

SALTS FOR USE IN ELECTROLYTE COMPOSITIONS OR AS ELECTRODE ADDITIVES

Here are described compounds for use as electrode additives or as salts in electrolyte compositions, and their methods of preparation. Also described are electrochemical cells comprising the compounds as electrode additives or as salts in electrolyte compositions.

SALTS FOR USE IN ELECTROLYTE COMPOSITIONS OR AS ELECTRODE ADDITIVES

Here are described compounds for use as electrode additives or as salts in electrolyte compositions, and their methods of preparation. Also described are electrochemical cells comprising the compounds as electrode additives or as salts in electrolyte compositions.

Synthesis method of N-substituted maleimide using solid acid catalysts

The present invention relates to a synthesis method of N-substituted maleimides using a non-homogeneous solid acid catalyst, and particularly, a synthesis method of N-substituted maleimides with high synthesis yield by using a zirconium(IV) hydrogen phosphate as a catalyst, by which, the loss of the catalyst is minimized, the separation and recovering processes of the catalyst are simplified, in case when the activity of the separated and recovered catalyst is decreased, the complete regeneration of the catalyst is possible via washing or firing, and solvents that could be used during a washing process of the catalyst are not limited.

Synthesis method of N-substituted maleimide using solid acid catalysts

The present invention relates to a synthesis method of N-substituted maleimides using a non-homogeneous solid acid catalyst, and particularly, a synthesis method of N-substituted maleimides with high synthesis yield by using a zirconium(IV) hydrogen phosphate as a catalyst, by which, the loss of the catalyst is minimized, the separation and recovering processes of the catalyst are simplified, in case when the activity of the separated and recovered catalyst is decreased, the complete regeneration of the catalyst is possible via washing or firing, and solvents that could be used during a washing process of the catalyst are not limited.

CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME

Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

PRODUCTION METHOD OF MALEIMIDE

An object is to provide a method for easily producing maleimide (MI) in which trace amounts of residual acid components as impurities in a crude MI are efficiently reduced, that is, the acid value is sufficiently reduced. <1> A method for producing purified MI, comprising reducing an acid value of crude MI by 50% or more, by adding carbodiimide (CDI) to a solution comprising the crude MI to react an acid component in the crude MI with the CDI. <2> The method for producing purified MI, comprising adding 0.5% by mass or more and 8% by mass or less of the CDI with respect to a mass of the crude MI for reaction. <3> The method for producing purified MI, wherein the CDI is N,N-diisopropyl carbodiimide (DIC). <4> The method for producing purified MI, comprising removing a urea derivative of the CDI (CDI-U) by-produced when reacting the acid component in the crude MI with the CDI.

PRODUCTION METHOD OF MALEIMIDE

An object is to provide a method for easily producing maleimide (MI) in which trace amounts of residual acid components as impurities in a crude MI are efficiently reduced, that is, the acid value is sufficiently reduced. <1> A method for producing purified MI, comprising reducing an acid value of crude MI by 50% or more, by adding carbodiimide (CDI) to a solution comprising the crude MI to react an acid component in the crude MI with the CDI. <2> The method for producing purified MI, comprising adding 0.5% by mass or more and 8% by mass or less of the CDI with respect to a mass of the crude MI for reaction. <3> The method for producing purified MI, wherein the CDI is N,N-diisopropyl carbodiimide (DIC). <4> The method for producing purified MI, comprising removing a urea derivative of the CDI (CDI-U) by-produced when reacting the acid component in the crude MI with the CDI.

Production method of maleimide

An object is to provide a method for easily producing maleimide (MI) in which trace amounts of residual acid components as impurities in a crude MI are efficiently reduced, that is, the acid value is sufficiently reduced. <1> A method for producing purified MI, comprising reducing an acid value of crude MI by 50% or more, by adding carbodiimide (CDI) to a solution comprising the crude MI to react an acid component in the crude MI with the CDI. <2> The method for producing purified MI, comprising adding 0.5% by mass or more and 8% by mass or less of the CDI with respect to a mass of the crude MI for reaction. <3> The method for producing purified MI, wherein the CDI is N,N-diisopropyl carbodiimide (DIC). <4> The method for producing purified MI, comprising removing a urea derivative of the CDI (CDI-U) by-produced when reacting the acid component in the crude MI with the CDI.