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Showing posts with label giza. Show all posts
Showing posts with label giza. Show all posts

Wednesday 13 January 2016

Ponalrestat



CAS # 72702-95-5, Ponalrestat, Statil, Statyl, 3-[(4-Bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid
Ponalrestat
Phase III
An aldose reductase inhibitor potentially for the treatment of diabetes.
ICI-128436; MK-538; ICI-plc
CAS No.72702-95-5
Statil; Statyl;
3-[(4-Bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid

Statil™ (3-(4-bromo-2-fluorobenzyl)-4-oxo-3H-phthalazin-1-ylacetic acid)

Molecular FormulaC17H12BrFN2O3
Molecular Weight391.19
IC50:Aldose reductase: IC50 = 7 nM (bovine); Aldose reductase: IC50 = 16 nM (rat); Aldose reductase: IC50 = 21 nM (pig); Aldose Reductase: IC50 = 21 nM (human); Rattus norvegicus:

400 MHz 1H-NMR spectrum of the dosing solution containing Statil™; HOD, residual ...
str1
Medicinal Chemistry, 2009, Vol. 5, No. 5,
str1
Synthesis of ethyl 2-(3-oxo-1,3-dihydro-1-isobenzofurany liden)acetate (2) A solution of phthalic anhydride (1.0 equiv.) and ethyl 2- (1,1,1-triphenyl-5 -phosphanylidene)acetate (1.1 equiv.) in 300 ml of dichloromethane (DCM) was refluxed for 3 hr. DCM was removed by vacuum at 40-50 o C. 2×150 ml of hexane was added to the resulting sticky solid, stirred for 10 min and the un-reacted 2-(1,1,1-triphenyl-5 -phosphanylidene)acetate was removed by filtration. The organic solvent was removed under vacuum and the resulting crude semisolid was taken to next step without further purification. Yield: 84%. 1 H-NMR CDCl3; (ppm): 1.1 (t, 3H), 4.2 (q, 2H), 6.0 (s, 1H), 7.6 (t, 1H), 7.7 (t, 1H), 7.8 (d, 1H), 8.9 (d, 1H). S
Synthesis of ethyl 2-(4-oxo-3,4-dihydro-1-phthalazinyl) acetate (3) A mixture of 2 (1.0 equiv.), hydrazine hydrate (0.8 equiv) and PTSA (1.0 equiv.) was ground by pestle and mortar at room temperature for 8 min. On completion, as indicated by TLC, the reaction mixture was treated with water. The resultant product was filtered, washed with water and recrystallized from DMF to give 3 in high yields (86%).1 H-NMR CDCl3; (ppm): 1.1 (t, 3H), 3.9 ( s, 2H), 4.1 (q, 2H), 7.6
Synthesis of 2-[3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4- dihydro-1-phthalazinyl]acetic acid (4)
A mixture of 3 (1.0 equiv.), NaOH (5.0 equiv.), and THF was stirred for 30 min at 40-50 o C. 4-bromo-1-bromomethyl-2-fluoro benzene (1.1 equiv.) was added to the reaction mixture and stirred for 2 hr at 50-60 o C. Water was added to the reaction mixture and stirred at room temperature for 1 hr. pH was adjusted to 2-3 using cold acetic acid. THF was removed and the aqueous phase was extracted with ethyl acetate (2×50 ml), washed with brine, dried over sodium sulphate and evaporated. The solid was crystallized with methanol to give 4 with 54 % yield.
1H-NMR (DMSOd6); (ppm): 3.98 (s, 2H), 5.3 (s, 2H), 7.17 (t, 1H), 7.35 ( dd, 1H, J1= 8.0, J2= 1.6), 7.55 (dd, 1H, J1= 8.0, J2= 1.6), 7.87 (t, 1H), 7.9 (t, 1H), 7.95 (t, 1H0, 8.29 (d, 1H).
str1

///////////Ponalrestat, ICI-128436, MK-538, ICI-plc,
C1=CC=C2C(=C1)C(=NN(C2=O)CC3=C(C=C(C=C3)Br)F)CC(=O)O



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Department of Pharmaceutics
Cairo, Giza, Egypt
Map of Cairo University Department of Pharmaceutics Cairo, Giza, Egypt


Cairo, Giza, Egypt




//////Cairo, Giza, Egypt,

Sunday 29 November 2015

(S)-tert-Butyl 2-(benzylcarbamoyl)pyrrolidine-1-carboxylate





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 (S)-tert-Butyl 2-(benzylcarbamoyl)pyrrolidine-1-carboxylate










Boc-L-proline
Boc-L-Proline: Boc-Pro-OH, N-(tert-Butoxycarbonyl)-L-proline; (15761-39-4)

benzylamine
Benzylamine: α-Aminotoluene; (100-46-9)

IR (neat) 3310, 2976, 2871, 1682, 1652, 1526, 1393, 1370, 1157, 1127, 766, 724, 693 cm-1. mp 124-125 °C.  




1H NMR (600 MHz, d-6 DMSO)

Major rotamer δ: 1.28 (s, 6 H), 1.41 (s, 3 H), 1.67 - 1.90 (m, 3 H), 2.04 - 2.18 (m, 1 H), 3.25 - 3.32 (m, 1 H), 3.36 - 3.43 (m, 1 H), 4.08 (dd, J = 8.6, 3.1 Hz, 1 H), 4.21 (dd, J = 14.0, 5.9 Hz, 1 H), 4.34 (dd, J = 14.0, 5.9 Hz, 1 H), 7.20-7.34 (m, 5 H), 8.39 (t, J = 5.9 Hz, 1 H).

Minor rotamer δ: 1.28 (s, 6 H), 1.41 (s, 3 H), 1.67 - 1.90 (m, 3 H), 2.04 - 2.18 (m, 1H), 3.25 - 3.32 (m, 1 H), 3.36 - 3.43 (m, 1 H), 4.12 (dd, J = 8.6, 3.1 Hz, 1 H), 4.19 (dd, J = 14.0, 5.9 Hz, 1 H), 4.34 (dd, J = 14.0, 5.9 Hz, 1 H), 7.20-7.34 (m, 5 H), 8.34 (t, J = 5.9 Hz, 1 H).  

1H NMR (600 MHz, DMSO, 60 °C) δ: 1.29 (s, 9 H), 1.67 - 1.91 (m, 2 H), 1.99 - 2.20 (m, 1 H), 3.29 (dt, J = 10.5, 6.8 Hz, 1 H), 3.38 (ddd, J = 10.5, 7.5, 5.1 Hz, 1 H), 4.10 (s, 1 H), 4.21 (dd, J = 14.9, 6.0 Hz, 1 H), 4.31 (dd, J = 14.9, 6.0 Hz, 1 H), 7.20 (t, J = 6.8 Hz, 1 H), 7.23 - 7.31 (m, 4 H), 8.16 (s, 1 H).


13C NMR (150 MHz, d-6 DMSO)




Major rotamer δ: 23.6, 28.4, 31.6, 42.5, 47.0, 60.4, 78.9, 127.8, 128.6, 140.1, 153.8, 172.9;

Minor rotamer δ: 24.5, 28.66, 30.5, 42.3, 47.2, 60.3, 79.1, 127.0, 127.19, 127.3, 140.1, 154.2, 172.7.

HRMS m/z calcd for C17H25N2O3 [M + H]+: 305.1860; Found: 305.1856. Anal. calcd for C17H24N2O3: C, 67.08; H, 7.95; N, 9.20; Found: C, 67.02; H, 7.89; N, 9.04.

Chiral HPLC AD-H column, 90:10 isohexane:2-PrOH, flow 0.7 mL/min, 30 °C, retention time 18.54 min (Retention times for racemic sample = 7.16 min and 19.93 min).








 

Le Meridien Pyramids Hotel  below

 


The Pyramids at Night, #Cairo

#Travelpics #Egypt #Travel


 

 

 Great Pyramids of Giza #Egypt
 
 
It's Not A Land On Earth , It's A Paradise In Heaven

#Giza #Pyramids #Egypt 




 
 
In the shadow of the Pyramids: the Nazlet El-Seman district in #Egypt's #Giza.

[Photo by Roger Anis from Everyday Egypt]



 
 
The Benben stone was a sacred stone in the solar temple of #Heliopolis. It was the location on which the first rays of the sun fell, is thought to have been the prototype for later obelisks, and the capstones of the great #pyramids were based on its design and dimensions. It was on this stone that the Phoenix or Benu Bird would return every 12.594 years.

#Egypt #Visit_Egypt #Travelpics #Travel
 

 

 


 

 
 
A beautiful morning with blue skies at the Pyramids of #Giza today in #Egypt.

Where are you spending your morning?



 

 
 
#Sphinx with #Pyramids #Egypt

 


 

 
 
Egypt - Pyramids view from Mena House Hotel rooms, Giza

 
 

 

 

 


 
 
 

 


 






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