DR ANTHONY MELVIN CRASTO,WorldDrugTracker, helping millions, A 90 % paralysed man in action for you, I am suffering from transverse mylitis and bound to a wheel chair, With death on the horizon, nothing will not stop me except God................DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 25Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK GENERICS at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution
Showing posts with label EDOXABAN INTERMEDIATE. Show all posts
Showing posts with label EDOXABAN INTERMEDIATE. Show all posts

Wednesday 2 September 2015

EDOXABAN INTERMEDIATE, 2-amino-5-methyl-4,5,6,7-tetrahydro thiazolone [5,4-c] pyridine




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ENDOXABAN





2-amino-5-methyl-4,5,6,7-tetrahydro thiazolone [5,4-c] pyridine 




(Reference Example 1) 2-amino-5-methyl-4,5,6,7-tetrahydro thiazolone [5,4-c] pyridine (1-n) (The method described in WO 2005/047296 Pamphlet )
[0091]
[Of 35]  in 2-PrOH (1.44L) solution was heated to 50 ℃ 1- methyl-4-piperidone (180.0g), 2-PrOH (360mL) solution of cyanamide (67.0g), and sulfur powder (51.0 g) it was added. Pyrrolidine (13.3mL) was added to the reaction mixture, after stirring for 2 hours at 50 ℃, followed by stirring overnight and allowed to cool to room temperature.  The reaction mixture was cooled to 10 ℃ less in an ice water bath and stirred for 1 hour at the same temperature. Is filtered and the precipitated crystals were washed with 2-PrOH (540mL), the title compound was dried under reduced pressure at 40 ℃ (209.9g, 78%) was obtained.



[0092]
1 H-NMR (CDCl 3 ) ppm: 4.86 (Br, 2H), 3.47-3.46 (t, 2H, J = 1.9 Hz), 2.78-2.71 (M, 2H), 2.71-2.65 (M, 2H), 2.47 . (s, 3H)
MS (FAB) M / z: 170 (M + H) +
elemental analysis: C 7 H 11 N 3 as S,
 theoretical value: C, 49.68; H, 6.55; N, 24.83; S, 18.95
 measured value: C, 49.70; H, 6.39; N, 24.91; S, 19.00.




 

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