The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) CC coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a hydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.

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Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

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Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

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The present invention relates to a preparation method of a long-chain compound, which includes the following steps: (1) carrying out condensation reaction on HR.sub.2 and R.sub.5N-Glu(OR.sub.4)OR.sub.3, wherein, R.sub.3 is a carboxyl protecting group, R.sub.4 is a carboxyl activating group, and R.sub.5 is an amino protecting group; obtaining a compound of formula II; (2) removing carboxyl protecting group R.sub.3 and amino protecting group R.sub.5 of the compound shown in formula II to obtain a compound of formula III; (3) carrying out condensation reaction on the compound shown in formula III and ##STR00001##
to obtain a compound shown in formula I. The method reduces the time of deprotection, and all the reactions can be carried out in a solvent with low boiling point. The post-processing requires only simple washing and recrystallization to obtain the product with higher purity, so the method is suitable for large-scale production.

This invention relates to a novel chemical process for the synthesis of N-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.

This invention relates to a novel chemical process for the synthesis of N-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer. ##STR00001##

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer. ##STR00001##

A method for producing a 1-(acyloxy)alkyl carbamate derivative (III), using a fluorous alkyl carbonate derivative (I), and a fluorous alkyl carbonate derivative (I) and a method for producing the same. In the formula, R.sup.1 represents C.sub.1-C.sub.4 alkyl group or a C.sub.3-C.sub.6 cycloalkyl group, R.sup.2 represents a C.sub.1-C.sub.4 alkyl group or a hydrogen atom, and A represents a fluorous alkyl group (wherein the fluorous alkyl group represents a C.sub.2-C.sub.11 alkyl group in which 40% or more of the hydrogen atoms are replaced by fluorine atoms).

A method for producing a 1-(acyloxy)alkyl carbamate derivative (III), using a fluorous alkyl carbonate derivative (I), and a fluorous alkyl carbonate derivative (I) and a method for producing the same. In the formula, R.sup.1 represents C.sub.1-C.sub.4 alkyl group or a C.sub.3-C.sub.6 cycloalkyl group, R.sup.2 represents a C.sub.1-C.sub.4 alkyl group or a hydrogen atom, and A represents a fluorous alkyl group (wherein the fluorous alkyl group represents a C.sub.2-C.sub.11 alkyl group in which 40% or more of the hydrogen atoms are replaced by fluorine atoms).