Selection of boron reagents for Suzuki-Miyaura coupling

Selection of boron reagents for Suzuki-Miyaura coupling


Chem. Soc. Rev.
, 2014, Advance Article
DOI: 10.1039/C3CS60197H, Review Article

Alastair J. J. Lennox, Guy C. Lloyd-Jones
School of Chemistry, University of Edinburgh, West Mains Road, Edinburgh, EH9 3JJ, UK
This review analyses the general physical and chemical properties of the seven main classes of boron reagent that have been employed for SM coupling
Suzuki–Miyaura (SM) cross-coupling is arguably the most widely-applied transition metal catalysed carbon–carbon bond forming reaction to date. Its success originates from a combination of exceptionally mild and functional group tolerant reaction conditions, with a relatively stable, readily prepared and generally environmentally benign organoboron reagent. A variety of such reagents have been developed for the process, with properties that have been tailored for application under specific SM coupling conditions. This review analyses the seven main classes of boron reagent that have been developed. The general physical and chemical properties of each class of reagent are evaluated with special emphasis on the currently understood mechanisms of transmetalation. The methods to prepare each reagent are outlined, followed by example applications in SM coupling.

A new method for synthesising model lignin oligomers will help scientists turn plant matter into biofuel

Green Chemistry International

Lignin is a complex and random polymer. This representative substructure shows some of the common linkages in lignin

A new method for synthesising model lignin oligomers will help scientists turn plant matter into biofuel

http://www.rsc.org/chemistryworld/2013/10/model-lignin-oligomers-biofuel

Unlike cellulose, a plant cell wall component with a repeating polymer structure, lignin is a complex and random polymer. The chemical units are linked by different connectivities, so one single process cannot attack all of these bonds. Previously, monomers and dimers were used to model chemical linkages of lignin, but were too simple for the study of lignin itself. More complex trimers, tetramers and hexamers have been synthesised, but with inefficient, low-yielding methods.  read all at   http://www.rsc.org/chemistryworld/2013/10/model-lignin-oligomers-biofuel

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Improved Continuous Flow Processing: Benzimidazole Ring Formation via Catalytic Hydrogenation of an Aromatic Nitro Compound

Figure

Improved Continuous Flow Processing: Benzimidazole Ring Formation via Catalytic Hydrogenation of an Aromatic Nitro Compound

Chemical Process Research and Development, Teva Pharmaceuticals, 383 Phoenixville Pike, Malvern, Pennsylvania 19355, United States
Org. Process Res. Dev., Article ASAP
Publication Date (Web): August 6, 2013 (Article)
DOI: 10.1021/op400179f
 In the development of a new route to bendamustine hydrochloride, the API in Treanda, the key benzimidazole intermediate 5 was generated via catalytic heterogeneous hydrogenation of an aromatic nitro compound using a batch reactor. Because of safety concerns and a site limitation on hydrogenation at scale, a continuous flow hydrogenation for the reaction was investigated at lab scale using the commercially available H-Cube. The process was then scaled successfully, generating kilogram quantities on the H-Cube Midi. This flow process eliminated the safety concerns about the use of hydrogen gas and pyrophoric catalysts and also showed 1200-fold increase in space–time yield versus the batch processing.

Epratuzumab

New Drug Approvals

Epratuzumab

Epratuzumab is a humanised anti-CD22 monoclonal antibody under investigation (clinical development phase III) for its efficacy in SLE. CD22 is a B cell specific surface protein that is considered to be involved in B cell function.

Expected indicationSystemic lupus erythematosus
R&D stagePhase 3 ongoing (started in December 2010)
Next milestonePhase 3 results (H1 2014)
Quick facts

Epratuzumab is a humanized monoclonal antibody. Potential uses may be found inoncology and in treatment of inflammatory autoimmune disorders, such as lupus (SLE).[1][2] The manufacturers in August 2009 announced success in early trials against SLE.[3]

Epratuzumab binds to the glycoprotein CD22 of mature and malignant B-cells.

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ONE LAKH VIEWS ON ALL BLOGS—DR ANTHONY CRASTO

New Drug Approvals

DR ANTHONY MELVIN CRASTO Ph.D

WORLDDRUGTRACKER

ANNOUNCING ONE LAKH PLUS VIEWS ON ALL BLOGS- DR ANTHONY CRASTO

SEE ALSO

DR ANTHONY MELVIN CRASTO, Worlddrugtracker, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India, in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK- GENERICS LTD, Research centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now sSanofi, Searle India ltd, now Rpg lifesciences, etc. he is now helping millions…

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