DRUG SPOTLIGHT…LEVETIRACETAM

New Drug Approvals

LEVETIRACETAM, etiracetam

(-)-(S)-α-ethyl-2-oxo-1-pyrrolidine acetamide

(−)-(S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide

CAS…102767-28-2

(aS)-a-Ethyl-2-oxo-1-pyrrolidineacetamide
Names: 2(S)-(2-oxopyrrolidin-1-yl)butyramide
Manufacturers’ Codes: UCB-L059; SIB-S1
Trademarks: Keppra (UCB)
FDA UNII: 44YRR34555
MF: C8H14N2O2
MW 170.21
Percent Composition: C 56.45%, H 8.29%, N 16.46%, O 18.80%

Crystals from ethyl acetate, mp 117°. [a]25D -90.0° (c = 1 in acetone). Soly (g/100 ml): water 104.0; chloroform 65.3; methanol 53.6; ethanol 16.5; acetonitrile 5.7. Practically insol in n-hexane. LD50 in male mice, male rats (mg/kg): 1081, 1038 i.v. (Gobert, 1990).

Mp: mp 117°C

O’Neil, M.J. (ed.). The Merck Index – An Encyclopedia of Chemicals, Drugs, and Biologicals. 13th Edition, Whitehouse Station, NJ: Merck and Co., Inc., 2001., p. 978
Optical Rotation: [a]25D -90.0° (c = 1 in acetone)
Specific optical rotation: -90 deg at 25 deg C/D (c = 1 in acetone)
Toxicity data: LD50 in male mice, male rats (mg/kg): 1081, 1038 i.v. (Gobert, 1990)
Therap-Cat: Anticonvulsant.
Very…

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Temsirolimus

New Drug Approvals

TEMSIROLIMUS

Proline CCI-779

Torisel, NCGC00167518-01

LAUNCHED 2007

PFIZER

  • CCI 779
  • CCI-779
  • HSDB 7931
  • Temsirolimus
  • Torisel
  • UNII-624KN6GM2T
  • WAY-CCI 779

Inhibits mTOR protein

For the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma.

An ester analog of rapamycin. Temsirolimus binds to and inhibits the mammalian target of rapamycin (mTOR), resulting in decreased expression of mRNAs necessary for cell cycle progression and arresting cells in the G1 phase of the cell cycle. mTOR is a serine/threonine kinase which plays a role in the PI3K/AKT pathway that is upregulated in some tumors

(1R,2R,4S)-4-{(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontin-3-yl]propyl}-2-methoxycyclohexyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate

cas 162635-04-3 

Temsirolimus is an…

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Chiral Tin Participates in Radical Cyclizations

 

Chiral tin hydrides generate radicals and transfer chirality in the cyclization of aldehydes
This offers an insight for the future design of catalytic asymmetric radical reactions.

Read more

http://www.chemistryviews.org/details/ezine/5446641/Chiral_Tin_Participates_in_Radical_Cyclizations.html

Rapid Wolff-Kishner reductions in a silicon carbide microreactor

Green Chem., 2013, Advance Article
DOI: 10.1039/C3GC41942H, Paper
Stephen G. Newman, Lei Gu, Christoph Lesniak, Georg Victor, Frank Meschke, Lahbib Abahmane, Klavs F. Jensen
Wolff-Kishner reductions are performed continuously in a silicon carbide microreactor. Short reactions times and safe operation are achieved, giving high yields without reactor corrosion issues using just 1.5 equivalents of hydrazine.

Rapid Wolff-Kishner reductions in a silicon carbide microreactor

http://pubs.rsc.org/en/Content/ArticleLanding/2013/GC/C3GC41942H?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

Wolff–Kishner reductions are performed in a novel silicon carbide microreactor. Greatly reduced reaction times and safer operation are achieved, giving high yields without requiring a large excess of hydrazine. The corrosion resistance of silicon carbide avoids the problematic reactor compatibility issues that arise when Wolff–Kishner reductions are done in glass or stainless steel reactors. With only nitrogen gas and water as by-products, this opens the possibility of performing selective, large scale ketone reductions without the generation of hazardous waste streams