8-Oxo-5-aza-spiro[2.5]octane-5-carboxylic acid benzyl ester,

str2

1H NMR PREDICT OF TITLE COMPD

…………………………………
13C NMR PREDICT

……………….

8-Oxo-5-aza-spiro[2.5]octane-5,7-dicarboxylic acid 5 benzyl ester 7 methyl ester
COMPD 5

SYNTHESIS CONSTRUCTION BY WORLDDRUGTRACKER………EXCLUSIVE

 

सुकून उतना ही देना प्रभू, जितने से जिंदगी चल जाये। औकात बस इतनी देना, कि औरों का भला हो जाये।
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09b37-misc2b027LIONEL MY SON
He was only in first standard in school when I was hit by a deadly one in a million spine stroke called acute transverse mylitis, it made me 90% paralysed and bound to a wheel chair, Now I keep him as my source of inspiration and helping millions, thanks to millions of my readers who keep me going and help me to keep my son happy
सुकून उतना ही देना प्रभू, जितने से
जिंदगी चल जाये।
औकात बस इतनी देना,
कि औरों का भला हो जाये।

 

////////////

Functionalized aryl-β-C-glycoside synthesis by Barbier-type reaction using 2,4,6-triisopropylphenyllithium

 

Kiyomi Ohba, Yuichi Koga, Sumihiro Nomura, and Masaya Nakata

“Functionalized aryl-β-C-glycoside synthesis by Barbier-type reaction using 2,4,6-triisopropylphenyllithium”
Tetrahedron Letters, 2015, 56, 1007–1010.

http://www.sciencedirect.com/science/article/pii/S0040403915000696

We developed an efficient synthetic route for functionalized aryl-β-C-glycosides, which are difficult to prepare by conventional methods. An aryl halide having an ester, cyano, or carbonyl group was treated with 2,4,6-triisopropylphenyllithium in the presence of a δ-lactone (Barbier-type reaction conditions) to afford a coupling product. The following deoxygenation gave the desired aryl-β-C-glycoside in good yield.

  • a Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation, 1000 Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan
  • b Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan

keywords

  • C-Glycoside;
  • Aldonolactone;
  • Barbier-type reaction;
  • Halogen–metal exchange reaction;
  • 2,4,6-Triisopropylphenyllithium

सुकून उतना ही देना प्रभू, जितने से जिंदगी चल जाये। औकात बस इतनी देना, कि औरों का भला हो जाये।
DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE

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09b37-misc2b027LIONEL MY SON
He was only in first standard in school when I was hit by a deadly one in a million spine stroke called acute transverse mylitis, it made me 90% paralysed and bound to a wheel chair, Now I keep him as my source of inspiration and helping millions, thanks to millions of my readers who keep me going and help me to keep my son happy
सुकून उतना ही देना प्रभू, जितने से
जिंदगी चल जाये।
औकात बस इतनी देना,
कि औरों का भला हो जाये।

 

Solvent-free Mizoroki–Heck reactions and its application in the synthesis of Axitinib

Originally posted on Green Chemistry International:

A green method for the synthesis of a D-glucosamine-derived triazole@palladium catalyst is described. The synthesized catalyst containing a 2-pyridyl-1,2,3-triazole ligand was prepared via a click route in high yields and was explored in Heck cross-coupling reactions between different aryl halides and olefins under solvent-free conditions. The catalyst can be separated from the reaction mixture and reused at least six times with superior activity. In addition, using this protocol, the marketed drug Axitinib (antitumor) could be synthesized easily.

Graphical abstract: A novel d-glucosamine-derived pyridyl-triazole@palladium catalyst for solvent-free Mizoroki–Heck reactions and its application in the synthesis of Axitinib

A novel D-glucosamine-derived pyridyl-triazole@palladium catalyst for solvent-free Mizoroki–Heck reactions and its application in the synthesis of Axitinib

Chao Shen,ab  Hongyun Shen,b  Ming Yang,b  Chengcai Xiab and   Pengfei Zhang*b  


*Corresponding authors
aCollege of Biology and Environmental Engineering, Zhejiang Shuren University, Hangzhou 310015, China
bCollege of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou 310036, China

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Aqua Mediated One-Pot Synthesis of 2-Amino-tetrahydrobenzo[b]pyran Derivatives Catalyzed by Mg(NO3)2•6H2O

Originally posted on Green Chemistry International:

.

http://benthamscience.com/journal/abstracts.php?journalID=loc&articleID=121326

Aqua Mediated One-Pot Synthesis of 2-Amino-tetrahydrobenzo[b]pyran Derivatives Catalyzed by Mg(NO3)2•6H2O

Letters in Organic Chemistry

Volume: 11
Issue Number: 7
First Page: 475
Last Page: 479
Page Count: 5
DOI: 10.2174/1570178611666140401221534

Author(s): Boudjemaa Boumoud, Amina Debbache, Taoues Boumoud, Raouf Boulcina and Abdelmadjid Debache

Affiliation: Laboratoire de Synthese de Molecules d’ Interets Biologiques, Departement de Chimie, Faculte des Sciences Exactes, Universite Constantine 1, 25000 Constantine, Algerie.
Abstract

We describe herein a clean and efficient one-pot synthesis of 4H-benzo[b]pyran derivatives using dimedone, active methylene nitriles and aryl aldehyde via Knoevenagel condensation followed by Michael addition in the presence of Mg(NO3)2•6H2O as catalyst and water as a green solvent. The advantages of this method lie in its simplicity, low catalyst loading, cost effectiveness and easy handling. The present method also allows us to synthesize highly functionalized tetrahydrobenzo[b]pyran derivatives from simple…

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Controlling Residual Arylboronic Acids as Potential Genotoxic Impurities in APIs

Originally posted on DRUG REGULATORY AFFAIRS INTERNATIONAL:

Arylboronic acids, but not the corresponding deboronated arenes, recently have been found to be weakly mutagenic in microbial assays [1].  Hence arylboronic acids may be considered potentially genotoxic impurities, and controlling the levels of residual arylboronic acids in APIs could become a regulatory requirement.  The issues should be decided by toxicology studies for the specific arylboronic acids in question.

Several approaches have been successful in removing boronic acids.  Diethanolaminomethyl polystyrene (DEAM-PS) [2],[3] and immobilized catechol [4] have been used to scavenge boronic acids.  Complex formation with diethanolamine may solubilize residual boronic acids in mother liquors.  Since arylboronic acids ionize similarly to phenols, basic washes of an API solution may remove arylboronic acids.  A selective crystallization can purge an arylboronic acid from the API.

The best means to control residual aryl boronic acids in APIs at the ppm level may be to decompose them through deboronation.  Sterically hindered, electron-rich aryl boronates…

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ML-236B, Mevastatin (compactin)

Originally posted on New Drug Approvals:

Mevastatin2DCSD.svgMevastatin (compactin, ML-236B) is a hypolipidemic agent that belongs to the statins class.

It was isolated from the mold Penicillium citrinum by Akira Endo in the 1970s, and he identified it as a HMG-CoA reductase inhibitor,[1] i.e., a statin. Mevastatin might be considered the first statin drug;[2] clinical trials on mevastatin were performed in the late 1970s in Japan, but it was never marketed.[3] The first statin drug available to the general public was lovastatin.

In vitro, it has antiproliferative properties.[4]

A British group isolated the same compound from Penicillium brevicompactum, named it compactin, and published their results in 1976.[5] The British group mentions antifungal properties with no mention of HMG-CoA reductase inhibition.

High doses inhibit growth and proliferation of melanoma cells.[6]

Systematic (IUPAC) name
(1S,7R,8S,8aR)-8-{2-[(2

View original 1,294 more words