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Saturday 17 January 2015

(S)-N-(2-(6-Methoxy-2,3-dihydro-1H-inden-1-yl)ethyl)propionamide




(S)-N-(2-(6-Methoxy-2,3-dihydro-1H-inden-1-yl)ethyl)propionamide

1: [a]D20 10.0 (c, 0.20, EtOH); mp 76–77 deg C;

1H NMR (500 MHz, CDCl3): d1.15 (t, 3H, J = 7.5 Hz), 1.60 (m, 1H), 1.70 (m, 1H), 2.02 (m, 1H), 2.19 (q, 2H, J = 7.5 Hz), 2.32 (m, 1H), 2.76 (m, 1H), 2.85 (m, 1H), 3.11 (m,
1H), 3.41 (m, 2H), 3.79 (s, 3H), 5.48 (s, 1H), 6.71 (dd, 1H, J = 2.0 Hz, 8.5 Hz), 6.75 (s, 1H), 7.11 (d, 1H, J = 8.0 Hz).

13C NMR (100 MHz,DMSO–d6): d 173.7, 158.7, 148.1, 135.8, 124.9, 112.3, 109.2, 55.5, 42.7, 37.9, 34.8, 32.5, 30.6, 29.8, 9.9. EI-MS: 247 ([M]+); HR-MS 247.1572
([M]+, C15H21NO2; Calcd. 247.1571).

The enantiomeric excess of (S)-1 was determined by HPLC as >99.9% [column, CHIRALPAK AS-H
(4.6 mm 250 mm), room temperature; eluent, hexane-2-propanol-trifluoroacetic acid (90:10:0.1); flow rate, 1.0 mL/min; detect, 290 nm; tR
of (S)-1, 30.7 min; tR of (R)-1 (enantiomer of (S)-1), 37.1 min].

S.B. Yu et al. / Chinese Chemical Letters 22 (2011) 264–267
: wlu@chem.ecnu.edu.cn (W. Lu).
Synthesis of the key intermediate of ramelteon
Shan Bao Yu a, Hao Min Liu a, Yu Luo a, Wei Lu b,


*a Department of Chemistry, East China Normal University, Shanghai 200062, China

b Institute of Drug Discovery and Development, East China Normal University, Shanghai 200062, China

http://sat.ecnu.edu.cn/Uploadnews/20120213113859628.pdf
and

https://www.heterocycles.jp/newlibrary/downloads/PDF/22186/85/1



Yu Luo
Associate Professor
Department of Chemistry
Institute of Technology Department of Chemistry
Tel: 021-54345462
Office Hours: Monday to Saturday 9: 00-19: 00
Fax:
Home URL:
Office Location: Minhang Chemistry Building 535
E-mail: yluo@chem.ecnu.edu.cn
Mailing address: 500 Dongchuan Road, East China Normal University Minhang Campus Chemistry Building 535








Research

(1) small molecule medicinal chemistry research. Including anticancer drugs, anti-hepatitis drugs and hypoglycemic drug design, synthesis and pharmacological properties of
(2) study of drug synthesis and fine chemicals. Includes a plurality of anticancer drugs, vitamin D drugs, natural phospholipids, as well as new anti-HIV drugs condensing agent, amino acid synthesis Studies link like fine chemicals
(3) research initiative targeted drug delivery technology based on liposomes, microspheres, vesicles, etc.

Affiliations

Academic Achievements

Recently published research papers 
1. Chen, TJ; Luo Y*; Hu, YH; Yang, B; Lu W, European Journal of Medicinal Chemistry201364, 613-620
2. Zhang, X; Zhang, J; Tong, LJ; Luo, Y; Su, MB; Zhang, Y; Li, J; Lu, W*; Chen, Y*, Bioorganic & Medicinal Chemistry201321, 3240-3244.
3. Luo, P; Luo, Y; Huang, J; Lu, W; Luo, DJ; Yu, JH*, Liu, SY, Colloids and Surfaces B: Biointerfaces2013109, 167-175. 
4. Mei, TW; Luo, Y*, Feng, XJ; Lu, W*; Yang, B,  Tetrahedron201369, 2927 – 2932
5. Wu, QE; Du, F; Luo, Y; Lu, W; Huang, J; Yu, JH*; Liu, SY*, Colloids and Surfaces B: Biointerfaces2013105, 294-302. 
6. Yong, DW; Luo, Y; Du, F; Huang, J; Lu, W; Dai, ZY; Yu, JH*; Liu, SY*, 2013105, 31-36.
7. Chen, TJ; Huang, QQ; Luo, Y*, Hu, YH*, Lu, W, Tetrahedron Letters201354, 1401-1404.
8. Luo,Y; Yu, SB; T, LJ; H, QQ; Lu, W; Chen, Y. European Journal of Medicinal Chemistry201254, 281-286.
9. Feng, XJ; Mei YH; Luo, Y*; Lu W, Monatshefte fur Chemie - Chemical Monthly2012143 , 161-164
10. Yu, SB; Huang, QQ; Luo, Y*; Lu, W*, Journal of Organic Chemistry 201277, 713-717.
11. Song, Y; Yuan, W; Luo, Y*; Lu, W Chinese Chemical Letters 201223, 154-156.
12. Zhang, LJ; Luo, Y; Yu, SB; Lu, W*,  Journal of Heterocyclic Chemistry201249, 1254-1256
13. Luo, Y; Xiao, F; Qian, SJ; He, QJ; Lu, W*; Yang, B* Synthesis and Evaluation of Novel 5-a, ß-unsaturated sulfonyl-indolin-2-ones as Potent Cytotoxic Agents,MedChemCommun20112, 1054 - 1057
14. Luo, Y; Liu, HM; Su, MB; Sheng, L; Zhou, YB; Li, J*; Lu, W* Synthesis and Biological Evaluation of Piper Amide Analogues as HDAC Inhibitors, Bioorganic & Medicinal Chemistry Letters201121, 4844-4866
15. Zhang, LJ; Xia, WP; Wang, B; Luo, Y*; Lu, W*, Convenient Synthesis of Sorafenib and ItsDerivatives, Synthetic Communications201141, 3140-3146
16. Luo, Y; Xiao, F; Qian, SJ; Lu, W*, Yang, B, Synthesis and in vitro cytotoxic evaluation of some thiazolylbenzimidazole derivatives, European Journal of Medicinal Chemistry,201146, 417-422.
17. Luo, Y; Yao, JP; Yang, L; Feng, CL; Tang, W; Wang, GF; Zuo, JP*; Lu, W*, Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives, Arch. Pharm. Chem. Life Sci. 20112, 78–83
18. Yu, SB; Liu, HM; Luo, Y; Lu, W*, Synthesis of the key intermediate of ramelteon, Chinese Chemical Letters201122,264–267
19. Luo, Y; Yao, JP; Yang, L; Feng, CL; Tang, W; Wang, GF; Zuo, JP*; Lu, W*, Design and synthesis of novel benzimidazole derivatives as inhibitors, Bioorganic & Medicinal Chemistry201018, 5048-5055.
20. Liu, HY; Xia, WP; Luo, Y; Lu, W*, A novel synthesis of imatinib and its intermediates, Monatshefte fur Chemie - Chemical Monthly2010141, 907-911.
21. Yu, SB; Luo, Y; Liu, HY; Liu, HM; Lu, W*, Synthesis of the DE synthon of racemic camptothecin, Monatshefte fur Chemie - Chemical Monthly2010141, 245-249.
22. Wang, B; Zhang, LJ; Fu, KY; Luo, Y*; Lu, W; Tang, J, An Efficient Synthesis of 1,2,6,7-Tetrahydro-8H-indeno[5,4-b]furan-8-one, Organic Preparations and Procedures International200941, 309-314.

Granted patent
ZL201010137564.1; Synthesis method phosphatidylethanolamine
ZL200910049896.1; multi-substituted pyridone compound synthesis
ZL200910054400.X; key intermediate in the synthesis method for the preparation of camptothecin compounds
ZL200710066688.3; a water-soluble derivative of camptothecin and its preparation method and application
ZL200810034511.X; (2- cyano - isopropyl) - Preparation of 3,5-toluene
ZL200910114955.9; one kind morpholine-carboxylic acid amides of N, N- dimethyl-4- do
ZL200810042729.X; Synthesis of 1,2,6,7-tetrahydro -8H- indeno [5,4-b] furan-8-one Method

The research project
National Drug Discovery major projects a sub-topics,Shanghai Natural Science Foundation 1, the Ministry of Education funds a young teacher, the State Key Laboratory of Drug Research Fund 1, business cooperation projects 5



























 September 2014 to celebrate the 15th anniversary of Professor Lv Wei from previous teaching students gathering
15th anniversary party







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4-(trans-2-((R)-2-methylpiperazine-1 -carbonyl)cyclopropyl)benzamide

4-(trans-2-((R)-2-methylpiperazine-1 -carbonyl)cyclopropyl)benzamide
Figure imgf000037_0001
Intermediate B (849 mg, 2.19 mmol) was dissolved in DCM (10.0 mL). TFA
(5.00 mL) was added and the reaction mixture stirred at rt for 30 min. Volatiles were evaporated under reduced pressure to give a yellow gum. The crude material was used in the next step without purification. 

1H NMR (400 MHz, CD3OD) δ ppm 1 .33 (d, J=7.03 Hz, 3H) 1 .37-1 .52 (m, 3 H) 1 .65 (br. s., 1 H) 2.26-2.39 (m, 1 H) 2.51 (br. s., 1 H ) 3.1 1 (br. s., 1 H) 3.21 -3.45 (m, 4H) 7.27 (d, J=8.20 Hz, 2H) 7.81 (d, J=8.20 Hz, 2 H).

(E)-tert-butyl 3-(4-cyanophenyl)acrylate

(E)-tert-butyl 3-(4-cyanophenyl)acrylate
Figure imgf000041_0001
A flame-dried three-neck round-bottom flask equipped with a magnetic stirring bar, a thermometer, an addition funnel and a nitrogen inlet was charged with NaH (3.96 g, 94.7 mmol) and anhydrous THF (120 mL). Tertbutyldiethylphosphono acetate (23.2 mL, 94.7 mmol) dissolved in anhydrous THF (20 mL) was added dropwise via the addition funnel over a period of 30 min. After the completion of addition, the reaction mixture was stirred at rt for another 30 min. A solution of 4- cyanobenzaldehyde (1 1 .3 g, 86.1 mmol) dissolved in anhydrous THF (20 mL) was added to the reaction mixture dropwise via the addition funnel over a period of 30 min. After the end of the addition, the reaction mixture was stirred at rt for 1 h, then diluted with MTBE (200 mL) and sat. NH4CI (150 mL). The organic layer was separated, washed with 25 mL of H20 and 25 mL of sat. NH4CI, dried over MgS04, filtered and evaporated to dryness to give 20.0 g Intermediate G as a solid (100%). 

1H NMR (400 MHz, CDCI3) δ ppm 1 .56 (s, 9H) 6.47 (d, J=16 Hz, 1 H) 7.58 (d, J=16 Hz, 1 H) 7.61 (d, J=8 Hz, 2H) 7.68 (d, J=8 Hz, 2H)
http://www.google.com/patents/EP2536701A1?cl=en









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Alfred Nobel had the unpleasant surprise of reading his own obituary, titled The merchant of death is dead, in a French newspaper.
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(1 S, 2S)-2-(4-Bromo-phenyl)-cyclopropanecarboxylic acid

(1 S, 2S)-2-(4-Bromo-phenyl)-cyclopropanecarboxylic acid
Figure imgf000051_0001
To a stirred solution of (trans)-2-(4-bromophenyl)cyclopropanecarboxylic acid (6.52 g, 27.04 mmol), which can be prepared in accordance with the process set forth on page 82 of WO 2009/024823, in 400 ml of EtOH was added a solution of (R)-(+)-1 -(1 -Naphthyl)ethylamine (4.63g, 4.37 ml_, 27.04 mmol), in 1 00 ml of EtOH followed by 25 ml of H20. This was stirred at rt for about 4 h. The solid was collected by filtration and washed with 40 ml of cold EtOH/H20 (20/1 ) providing 3.18 grams of salt as a white solid (58 % recovery) equivalent to 1 .86 g of free acid. This was taken up in 2 N NaOH and extracted 5Xs with EtOAc. The aq. phase was placed on a rotary evaporator to remove the remaining EtOAc. The resulting clear solution was transferred to an erlenmeyer flask, cooled in an ice bath, and cone. HCI was added dropwise while stirring to pH 4. The resulting solid was collected by filtration providing 1 .63 g of Intermediate R. The product was analyzed by chiral SFC (UV detection) using isocratic method (mobile phase: 25% MeOH with 0.1 % DMEA, supercritical C02) on ChiralPak AD-H, 10 x 250 mm, 5 μιη particle size, giving an enantiomeric purity of >95%, Rt 3.88 min (isomer 1 ) and 4.79 min (isomer 2). 

1 H NM R (400 MHz, CDCI3) δ ppm 1 .37 (ddd, J=8.20, 6.64, 4.69 Hz, 1 H), 1 .67 (ddd, J=9.28, 5.08, 4.79 Hz, 1 H), 1 .87 (ddd, J=8.50, 4.69, 4.39 Hz, 1 H), 2.48-2.63 (m, 1 H), 6.87-7.06 (m, 2H), 7.37-7.46 (m, 2H).

http://www.google.com/patents/EP2536701A1?cl=en











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