169280-16-4

Upstream product

• 28509-24-2 tert-butylmethyl ether 
• 826-55-1 2-methyl-2-phenylpropionic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 140-29-4 phenylacetonitrile 
• 1195-98-8 2-methyl-2-phenylpropionitrile 
• 57625-74-8 methyl 2-methyl-2-phenylpropionate 
• 36293-05-7 2-methyl-2-phenylpropanoyl chloride 

Downstream Products

• 169280-21-1 2-[4-(4-chloro-butyryl)-phenyl]-2-methyl-propionic acid 
• 202189-78-4 Bilastine 
• 770-85-4 2-methyl-2-phenylbutan-3-one 
• 154477-54-0 2-[4-(4-Chloro-butyryl)-phenyl]-2-methyl-propionic acid, methyl ester 
• 154477-55-1 methyl 2-(4-(4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoate 

Relevant academic research and scientific papers

A new and competitive synthetic approach for an antihistamine agent, bilastine

Efforts towards the novel synthesis of second generation non-sedating antihistamine drug, Bilastine was described in this manuscript. This competitive synthetic approach involves the convergent synthesis of Bilastine via simple Friedel-Crafts acylation as an alternate for earlier reported Stille and Suzuki couplings. The selectivity in Friedel-Crafts acylation reaction with chloro acetyl chloride on different substituted arenes was studied and employed the best conditions for the synthesis of Bilastine. Further synthetic approach involves the deoxygenation of aryl ketone to corresponding alkane in single step and finally provides Bilastine with 39% of improved overall yields, utilizing simple and cost-effective reagents, suitable for kilogram scale synthesis.

Synthetic method of fexofenadine intermediate

The invention provides a synthetic method of a fexofenadine intermediate 2-[4-[4-[4-(hydroxybenzhydryl)-1-piperidyl]-butyryl]phenyl]-2- methylmethacrylate. The method comprises the following steps: methylation of phenylacetonitrile which is used as a raw material, basic hydrolysis, weinreb amidation reaction, Friedel-crafts reaction, acid hydrolysis, esterification and condensation. The method has the following advantages: raw materials and auxiliary materials are cheap and easily available; yield is high; cost is low; there is no meta-isomer; and the method is suitable for industrial production.

SOLID STATE FORMS OF 2-[4-(2-{4-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL]-1-PIPERIDINYL}ETHYL)PHENYL]-2-METHYLPROPANOIC ACID AND PROCESS FOR PREPARATION THEREOF

The present invention relates to solid state forms of 2-[4-(2-{4-[1 -(2-ethoxyethyl)- 1H-benzimidazol-2-yl] - 1 -piperidinyl } ethyl)phenyl]-2-methylpropanoic acid compound represented by the following structural formula- 1 and process for preparation the

6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepines derivatives as histamine H4 receptor ligands

The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.

NOVEL PROCESS FOR THE PREPARATION OF 2-[4-(2-{4-[1-(2-ETHOXYETHYL)-1H-BENZIMIDAZOL-2-YL]-1-PIPERIDINYL}ETHYL) PHENYL]-2-METHYLPROPANOIC ACID

The present invention relates to novel process for the preparation of 2-[4-(2-{4-[l-(2- ethoxyethyl)-lH-benzimidazol-2-yl]-l-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid represented by the following structural formula- 1. Formula- 1 The present invention also provides novel intermediate compounds useful for the preparation of compound of formula- 1.

A Weinreb amide approach to the synthesis of trifluoromethylketones

A novel route to access trifluoromethylketones (TFMKs) from Weinreb amides is reported. This represents the first documented case of the Ruppert-Prakash reagent (TMS-CF3) reacting in a constructive manner with an amide and enables synthesis of TMFKs without risk of over-trifluoromethylation.

Intermediates useful for the preparation of antihistaminic piperidine derivatives

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula whereinW represents —C(=O)— or —CH(OH)—;R1 represents hydrogen or hydroxy;R2 represents hydrogen;R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2;n is an integer of from 1 to 5;m is an integer 0 or 1;R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.

Intermediates useful for the preparation of antihistaminic piperidine derivatives

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula whereinW represents —C(=O)— or —CH(OH)—;R1 represents hydrogen or hydroxy;R2 represents hydrogen;R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2;n is an integer of from 1 to 5;m is an integer 0 or 1;R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.

Intermediates useful for the preparation of antihistaminic piperidine derivatives

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1represents hydrogen or hydroxy; R2represents hydrogen; R1and R2taken together form a second bond between the carbon atoms bearing R1and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1and R2are taken together to form a second bond between the carbon atoms bearing R1and R2or where R1represented hydroxy, m is an integer 0.

Intermediates useful for the preparation of antihistaminic piperidine derivatives

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents -C(=O)- or -CH(OH)-; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is -COOH or -COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are ta to form a second bond between the carbon R1 and R2 or where R1 represented hydroxy integer 0.