HEARD OF F-SOFOSBUVIR...CN103848877A

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.

 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.

DHAKA BANGLADESH

.

Steamers and ferries in Sadarghat Port

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WO 2015037587, PRI 724

STRUCTURE 4
4-(((6S,9S,9aS)-l-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro- 1 H-pyrazino[2, 1 -c] [ 1 ,2,4]triazin-6-yl)methyl)phenyl dihydrogen phosphate

STRUCTURE 5
(6S,9S,9aS)-N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-yImethyl)octahydro- 1 H-pyrazino[2, 1 -c] [ 1 ,2,4]triazine- 1 -carboxamide.
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WO-2015037587
Eisai Research Institute; PRISM Pharma Co Ltd
This method of producing 4-(((6S,9S)-l-(benzylcarbamoyl)-2,9-dimethyl-4,7-dioxo-8-(quinoline-8-ylmethyl) octahy- dro-1H-pyrazino[2,1-c][1,2,4]triazine-6-yl)methyl) phenyl dihydrogen phosphate involves a step for adding a reaction solution (I) comprising (6S,9S)-N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinoline-8-ylmethyl) octahydro-1H-pyrazino[2,1-c] [I,z,4]triazine-1-carboxamide, triethylamine and a solvent to a reaction solution (2) comprising a phosphorylating agent and a solvent.
1
1H-NMR (600MHz, METHAN0L-d4) δ (ppm):1.15 (d, J=6 Hz, 3H), 2.65 (s, 3H), 3.12 (d, J=18 Hz, 1H), 3.35 (d, J=7 Hz, 2H), 3.48 (d, J=18 Hz,1H), 4.15 (m,1H), 4.32 (d, J=15 Hz, 1H), 4.40 (d, J=15 Hz, 1H), 5.33(d, J=16 Hz, 1H), 5.41(d, J=16 Hz, 1H), 5.44 (d, J=7 Hz, 1H), 5.64 (d, J=10 Hz, 1H), 7.07 (dd, J=9,1 Hz, 2H), 7.15 (d, J=9 Hz, 2H), 7.24 (t, J=7 Hz, 1H), 7.27 (d, J=7 Hz, 2H), 7.34 (t, J=8 Hz, 2H), 7.55 (d d, J=8, 4 Hz, 1H), 7.60 (brd, J=6 Hz, 1H), 7.62 (dd, J=8, 7 Hz, 1H), 7.88 (dd, J=8,1 Hz, 1H), 8.38 (dd, J=8, 2 Hz, 1H), 8.90 (dd, J =4, 2 Hz, 1H).

.

PART A 

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PART B
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 PART C
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PART D
THIS PERCURSOR GIVES FINAL


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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.

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.

DHAKA BANGLADESH

.

Steamers and ferries in Sadarghat Port

Kawran Bazar

.

Dry fish sellers at the Karwan Dry Fish Market (Bazar), Dhaka, Bangladesh.

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