Part-I - Controller General of Patents Designs and Trademarks

(12) PATENT APPLICATION PUBLICATION (21) Application No.1384/CHE/2011 A
(19) INDIA
(22) Date of filing of Application :21/04/2011 (43) Publication Date : 21/06/2013
(54) Title of the invention : A PROCESS FOR PREPARATION OF 4-FLUORO- α - [2-METHYL-1-OXOPROPYL] - γ -OXO-
N- β - DI HENYLBENZENE BUTANE AMIDE
(51) International classification :C07C
(31) Priority Document No :NA
(32) Priority Date :NA
(33) Name of priority country :NA
(86) International Application No
:NA
Filing Date
:NA
(87) International Publication No : NA
(61) Patent of Addition to Application Number :NA
Filing Date
:NA
(62) Divisional to Application Number
:NA
Filing Date
:NA
(71)Name of Applicant :
1)VIJAYASRI ORGANICS LIMITED
Address of Applicant :PLOT NO 39, 1ST FLOOR,
VIJAYASRI ENCLAVE VIKASPURI, HYDERABAD - 500
038 Andhra Pradesh India
(72)Name of Inventor :
1)SRIVATSAVAYI JAGAPATHI RAJU
2)POTHUKUCHI SAIRAM
3)RANI SRINIVASA SASTRY
4)CHIKKA MALLIKARJUNA RAO
5)CHEEKATI CHIRANJEEVI
6)GUTTHI MALLIKARJUNA RAO
7)SINGAVARAPU TRIMURTHULU
8)THIMMAIPALLY VENKAT REDDY
9)TADANKI VENKATESWARA RAO
(57) Abstract :
A process for preparation of 4-fluoro- α -[2-methyl-l-oxopropyl]-Y-oxo-N-β- diphenylbenzene butane amide also known as a
diketone intermediate of atorvastatin, completely devoid of impurities 3,4-difluoro- α -[2-methyl-l-oxopropyl]-y-oxo-n-βdiphenylbenzene
butane amide; methyl, 2{-2[-(4-fluorophenyl)-2-oxo-l-phenyl ethyl)] }-4-methyl-3-oxo pentanoate; 1,4-bis(4-
fluorophenyl)-2,3-diphenylbutane-l,4-dione, l-(4-fluorophenyl)-2-phenyl ethanone; 1-(4-fluorophenyl)-2-phenyl ethanone and
containing about 0.05% or less of 2-methyl-l-oxopropyl]-Ƴ-oxo-N-β- diphenylbenzene butane amide. In that process the said
diketone intermediate of formula 1 is obtained by maintaining temperature -25° C to 50° C during Friedel-Crafts acylation, in situ
halogenation of formula II in presence of a solvent and nucleophilic substitution from a compound of formula III with formula IV
in presence of a base.
No. of Pages : 35 No. of Claims : 16
The Patent Office Journal 21/06/2013 13783