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(12) PATENT APPLICATION PUBLICATION
(19) INDIA (21) Application No.: 1276/MUM/2004 A
(22) Date of filing of Application: 30/11/2004 (43) Publication Date: 09/06/2006
(54) Title of the invention: PROCESS FOR THE PREPARATION OF ACETYLENIC RETINOID
(51) International classification : A61K 31/56,
A61K 6/00,
C07D 413/06,
C07D 413/12
(31) Priority Document No : NIL
(32) Priority Date : NIL
(33) Name of priority country : NIL
(86) International Application No : NIL
and Filing Date : NIL
(87) International Publication No : NIL
(61) Patent of addition to :
Application No
NIL
(62)
Filed on : N.A.
Divisional to Application No : NIL
Filed on : N.A.
(57) Abstract: A process for the preparation of
acetylenic retinoid, ethyl-6-[2-(4,4dimethylthiochroman-6-yl)ethynyl]nicotinate,
a
compound of formula 1,
comprising, (a) cyclizing phenyl-3-methylbut-2enylsulfide,
a compound of formula 6, in presence of an
acid selected from sulfuric acid or p-toluenesulfonic
acid to yield 4,4-dimethylthiochroman, a compound of
formula 2; (b)acetylating the compound of formula 2, to
4,4-dimethyl-6-acetylthiochroman, a compound of
formula 3; (c) (i) reacting the compound of formula 3
with hydrazine; (ii) reacting resultant product of step (i)
with iodine; (iii) converting the resultant product of step
(ii) to 4,4-dimethyl-6-ethynyl thiochroman, a compound
of formula 4 and
(d) reacting the compound of formula 4 with ethyl-6halonicotinate,
a compound of formula 5,
(71) Name of Applicant:
SUN PHARMACEUTICAL
INDUSTRIES LTD.
Address of the Applicant:
ACME PLAZA, ANDHERI-KURLA
ROAD, ANDHERI (E), MUMBAI-400
059, MAHARASHTRA, INDIA.
(72) Name of the Inventor:
1. MR.JAIN CHIRAG NARENDRA
2. MR.VAGHELA MUKESH
NATHALAL
3. DR. REHANI RAJEEV BUDHDEV
4. DR.THENNATI RAJAMANNAR
Filed U/S 5(2) before The Patents
(Amendment) Act, 2005: NO
wherein X is C1 or Br, in presence of cuprous halide, a transition metal and inorganic base in an organic solvent.
Drawing Sheets: NIL
Total Pages: 45.
Fig. Nil
The Patent Office Journal 09/06/2006 10932