A Continuous Flow Chemistry Platform for Low Temperature Reactions

A low temperature reactor platform that facilitates metalation followed by electrophilic quenching, and related reactions under continuous flow-through conditions has been developed.

Pre-cooling loops are incorporated for all 3 reactor input streams and gaseous reagent inputs can be easily introduced by attaching a ‘tube-in’tube’ presaturation module.

All of the coil reactors and flow chemistry equipment described are are available from Uniqsis Ltd

ENZALUTAMIDE

Originally posted on New Drug Approvals:

Enzalutamide, MDV-3100
MDV3100 is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. MDV3100 (Enzalutamide) blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also induces tumour cell apoptosis, and has no agonist activity. Early preclinical studies also suggest that MDV3100 inhibits breast cancer cell growth.
1H NMR FROM THE NET

1H NMR PREDICT AND 13 C NMR PREDICT BELOW

COSY PREDICT

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PATENT
http://www.google.com/patents/WO2015063720A1?cl=en

Enzalutamide is chemically described as 4-{3-[4-cyano-3-(trifluoromethyl)phenyl] -5 ,5 -dimethyl-4-oxo-2-sulfanylideneimidazolidin- 1 -yl } -2-fluoro-N-methylbenzamide of Formula I.
FORMULA I
Processes for the preparation of enzalutamide are described in U.S. Publication Nos. 2007/0004753 and 2007/0254933 and PCT Publication Nos. WO 2007/127010, WO 2006/124118, and WO 2011/106570.
PCT Publication No. WO 2011/106570 discloses that the processes described in U.S. Publication Nos. 2007/0004753 and 2007/0254933 result in a 25% yield of…

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

str2

1H NMR PREDICT OF TITLE COMPD

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13C NMR PREDICT

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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।
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।

 

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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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Join me on google plus Googleplus

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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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