Showing posts with label CN103848877A. Show all posts
Showing posts with label CN103848877A. Show all posts

Thursday 9 April 2015

HEARD OF F-SOFOSBUVIR...CN103848877A


Figure CN103848877AD00083
F SOFOSBUVIR

1613739-48-2
L-​Alanine, N-​[[P(S)​,​2'R]​-​2'-​deoxy-​2',​5-​difluoro-​2'-​methyl-​P-​phenyl-​5'-​uridylyl]​-​, 1-​methylethyl ester
C22 H28 F2 N3 O9 P, 547.44

http://www.google.com/patents/CN103848877A?cl=en


Preparation of Comparative Example II of the compound of formula I
The present invention with reference to US20110251152A1 (Example 1) Preparation of the technical contents disclosed to give a compound of formula II.

Figure CN103848877AD00071
 δ (1HNMR, DMS0_d6): 1.25 (d, J = 22.4Hz, 3H), 3.64 (m, 1H), 3.83 (m, 3H), 5.27 (m, 1H), 5.64 (m, 1H), 5.66 (m, 1H), 5.97 (d, J = 18.8Hz, 1H), 9.96 (d, J = 8.0Hz, 1H), 11.45 (s, lH) ppm; δ (19FNMR, DMS0-d6): - 159.9 (s) ppm; MS: 261 (MH +) o
 The preparation of the usual 2Sofosbuvir
The present invention with reference to US20110251152A1 (Example 10_7) Preparation of the technical contents disclosed in the Sofosbuvir.

Figure CN103848877AD00081
 δ (1HMlR, DMS0_d6): 1.15 (d, J = 6.0Hz, 6H), 1.22 (d, J = 6.4Hz, 3H), 1.25 (d, J = 22.3Hz, 3H), 3.80-4.00 ( m, 3H), 4.11 (m, 1H), 4.42 (m, 1H), 4.52 (m, 1H), 5.00 (m, 1H), 5.30 (d, J = 8.0Hz, 1H), 6.20 (m, 1H ), 7.10-7.30 (m, 3H), 7.30-7.35 (m, 2H), 7.46 (d, J = 8.2Hz, 1H), 11.45 (s, 1H) ppm; δ (19MMR, DMS0_d6): - 161.68 ( s) ppm; δ (31PNMR, DMS0-d6): 3.35 (s) ppm; MS: 530 (MH +) o
Preparation of Comparative Example 3 Compound of Formula III
The present invention with reference to Chinese Patent Application CN201310098009.6 (Example 4) Preparation of the technical contents disclosed to give a compound of formula III.

Figure CN103848877AD00082
δ (1HNMR, DMS0_d6): 1.35 (d, J = 22.4Hz, 3H), 3.71 (m, 1H), 3.98 (m, 1H), 4.13 (m, 1H), 4.93 (m, 1H), 5.72 (m, 1H), 6.05 (d, J = 20.4Hz, 1H), 7.76 (d, J = 6.8Hz, 1H), 11.88 (s, lH) ppm; δ (19FNMR, DMS0-d6): - 168.06 (s), -176.03 (s) ppm; MS: 279 (MH +) o
 The preparation of the usual 4F_Sofosbuvir
The present invention with reference to Chinese Patent Application CN201310098009.6 (Example 5) was prepared technical contents disclosed to Ij F-Sofosbuvir0

Figure CN103848877AD00083
δ (1HMlR, DMS0-d6): 1.13 (d, J = 6.0Hz, 6H), 1.22 (d, J = 6.4Hz, 3H), 1.25 (d, J = 22.3Hz, 3H), 3.80- 4.00 (m, 3H), 4.11 (m, 1H), 4.42 (m, 1H), 4.52 (m, 1H), 5.00 (m, 1H), 6.20 (m, 1H), 7.10-7.30 (m, 3H) , 7.30-7.35 (m, 2H), 7.46 (d, J = 8.1Hz, 1H), 11.50 (s, lH) ppm; δ (19FNMR, DMS0-d6): - 161.68 (s), -167.58 (s) ppm; δ (31PNMR, DMS0_d6): 3.35 (s) ppm; MS: 548 (MH +).

Figure CN103848877AD00121



http://www.google.com/patents/CN103848876A?cl=en
A compound of the structure shown in formula I,
Figure CN103848876AC00021
Wherein, X is selected from F, Cl, Br, I of any one.










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