The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

##STR00001##

The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.

##STR00001##

Carbamate and beta-amino acid urea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used for imaging cells and tumors that express PSMA or for cancer radiotherapy. These compounds also can comprise a fluorescent dye and be used for imaging cells and tumors that express PSMA or for photodynamic therapy.

Carbamate and beta-amino acid urea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used for imaging cells and tumors that express PSMA or for cancer radiotherapy. These compounds also can comprise a fluorescent dye and be used for imaging cells and tumors that express PSMA or for photodynamic therapy.

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

The invention relates to an aqueous coating composition comprising a compound having reactive groups A, and a quaternary ammonium compound according to Formula I, II or III ##STR00001##
wherein R.sup.1 is an alkyl, alkenyl, alkylaryl or arylalkyl group having from 5 to 50 carbon atoms; R.sup.2 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.3 and R.sup.4 are alkylene groups having from 1 to 4 carbon atoms; R.sup.5 and R.sup.6 are H or C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.7 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.8 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.9 is H or a methyl group; Z is a substituent containing at least one reactive group B which is capable of reacting with the reactive group A; X.sup.− is an anion; y is 0 or 1; a is 0 or 1; and the sum of y and a is 1 or 2 and m is an integer from 1 to 30, preferably between 1 and 10, or between 2 and 6 n is an integer from 0-30, preferably between 1 and 10, or 2 and 6 T is a monomer unit; U is a monomer unit; V is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing hetero atoms; d is an integer between 1 and 5, preferably 1; e is an integer between 1 and 1000, preferably between 5 and 100; g is an integer between 1 and 100, preferably between 2 and 10; h is an integer between 1 and 5, preferably 2 or 3.

The invention relates to an aqueous coating composition comprising a compound having reactive groups A, and a quaternary ammonium compound according to Formula I, II or III ##STR00001##
wherein R.sup.1 is an alkyl, alkenyl, alkylaryl or arylalkyl group having from 5 to 50 carbon atoms; R.sup.2 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.3 and R.sup.4 are alkylene groups having from 1 to 4 carbon atoms; R.sup.5 and R.sup.6 are H or C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.7 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.8 is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing heteroatoms; R.sup.9 is H or a methyl group; Z is a substituent containing at least one reactive group B which is capable of reacting with the reactive group A; X.sup.− is an anion; y is 0 or 1; a is 0 or 1; and the sum of y and a is 1 or 2 and m is an integer from 1 to 30, preferably between 1 and 10, or between 2 and 6 n is an integer from 0-30, preferably between 1 and 10, or 2 and 6 T is a monomer unit; U is a monomer unit; V is a C.sub.1-C.sub.100 hydrocarbyl group, optionally containing hetero atoms; d is an integer between 1 and 5, preferably 1; e is an integer between 1 and 1000, preferably between 5 and 100; g is an integer between 1 and 100, preferably between 2 and 10; h is an integer between 1 and 5, preferably 2 or 3.

A method for esterification of one or more carboxylic acid groups in a compound containing one or more carboxylic acid groups wherein the esterification reagent is a diazo-compound of formula:

##STR00001##

wherein the R.sub.1 and R.sub.2 groups of the diazo compound are selected such that the corresponding organic compound of formula:

##STR00002##

exhibits a —C—H pKa value between 18 and 29 as measured in DMSO. Specific reagents and methods for esterification are provided. The esterification reagents provided exhibit high selectivity for esterification of carboxylic acid groups over reaction with amine, alcohol or thiol groups in the compound containing one or more carboxylic acid groups. The method can be used to selectively esterify carboxylic acid groups in peptides or proteins.