...
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
C
22 H
28 F
2 N
3 O
9 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.
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.
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.
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
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 +).
http://www.google.com/patents/CN103848876A?cl=en
A compound of the structure shown in formula I,
Wherein, X is selected from F, Cl, Br, I of any one.
P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.
P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.
P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.
COCK WILL TEACH YOU NMR
COCK SAYS MOM CAN TEACH YOU NMR
Join me on twitter
amcrasto@gmail.com
DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE
.png)
