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ChiroSolve Inc. 2065 Martin Ave, Suite 107, Santa Clara, CA 95050, USA ; Telephone: +1(408) 834-8597; Fax: +1(408) 351-7900;

July 2011 Newsletter, Vol 2, Issue 4   


News You Can Use    


Cyclopropyl Dihydro-Alkylthio-Benzyl-Oxopyrimidine

molecule 2


 Screening Kits to identify separation conditions
EnantioPrep to develop enantiomer
ScalePrep for method optimization
Chiral Resolution Services


Discovery of Chiral Cyclopropyl Dihydro-Alkylthio-Benzyl-Oxopyrimidine (S-DABO) Derivatives as Potent HIV-1 Reverse Transcriptase Inhibitors with High Activity Against Clinically Relevant Mutants (see more >>>)

First lupus drug in half a century approved BY: Heidi Ledford
(see more >>>)

On the origin of terrestrial homochirality for nucleosides and amino acids By: Ronald Breslow1 and Zhan-Ling Cheng
(see more >>>)


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Contact us at: ChiroSolve, Inc.
2065 Martin Ave. suite 107,
                      Santa Clara, CA 95050
                      Phone: +1(408) 834-8597
                      Fax: +1(408) 351-7900

Dear Chiral Chemistry Colleague,

Welcome back to the ChiroSolve Monthly Newsletter designed to bring insightful and timely information on trends and technology to innovators in Organic Chemistry.

We are very excited that our new product ENANTIOPREP that delivers pure enantiomer and defines chiral separation method within matter of days has been very well received by the research community. We have received many inquiries regarding the product and its applications. In response, we will be publishing number of articles and application notes. Please stay tuned. 

Special note: Our SCREEN kits and ENANTIOPREP kits will be featured in the upcoming Chemfiles (2011, Volume 11, number 3 ) by Sigma Aldrich, our valued distribution partner.

Resolution by diastereomeric crystallization - facts for chemists

Diastereomeric crystallization is a predominant technique employed during manufacturing to resolve any type of chiral compound (acid, base, alcohol, aldehyde, ketone, amino acid, etc.); mainly because of the robustness and consistency of the method and its cost-effective nature. This selective crystallization process begins with mixing racemate with a pure chiral resolving agent and an organic solvent.  After heating the mixture, the diastereomeric salt of one of the enantiomer crystallizes out, while the other enantiomeric salt stays in the filtrate. In most cases, after the desired enantiomer has been separated from the diastereomeric salt, the resolving agent is recovered and becomes available for reuse. By treating the crystallized salt with more solvent and repeating the crystallization, you can obtain increasingly pure enantiomer until target purity is obtained.

ChiroSolve utilizes diastereomeric crystallization technique in its products (SCREEN, ENANTIOPREP and SCALEPREP) and offers streamlined solutions with simple pre-defined step-by-step procedures to follow that consistently offer results within matter of days. Using these products you can
comprehensively identify and optimize a chiral resolution method (scalable to kilo quantities) and obtain pure enantiomer for initial pre-clinical studies or lead optimization.

Among the top-ten best selling drugs, the following drugs use diastereomeric crystallization during production.

  • Paroxetine with US$ B 3.3 sales is a selective serotonin reuptake inhibitor developed by Novo Nordisk’s subsidiary, Ferrosan, and licensed to SmithKline Beecham (now GlaxoSmithKline). It is sold under the name Paxil - the hydrochloride salt - used to treat depression, anxiety, and obsessive compulsive disorder. It is prepared by resolution using di-p-Toluoyl-Tartaric acid (-).

  • Clopidogrel or Plavix had annual sales of US$ 3B 2.9 is marketed by sanofi-synthelabo and Bristol-Meyer-Squibb. It is a platelet aggregation inhibitor - used as an antithrombotic agent for the reduction of cardiovascular events. The production of this material uses diastereomeric crystallization with Camphor sulfonic acid.

  • Setraline is an antidepressant that inhibits the uptake of seratonin in the central nervous system. It is marketed by Pfizer under the name Zoloft with annual sale of US $B2.7. It uses diastereomeric crystallization of the racemate by D-Mandelic acid.


First lupus drug in half a century approved

For more than 50 years, the autoimmune disease lupus has confounded drug developers. But a new therapy finally broke through that barrier yesterday when the US Food and Drug Administration (FDA) announced the approval of Benlysta (belimumab) for the treatment of systemic lupus erythematosus.

The greatly anticipated move heralded a step forward not only for belimumab's developers, but also for the many other experimental lupus therapies hot on the trail. "It's a very exciting time in lupus," says Richard Furie, a rheumatologist at the North Shore-Long Island Jewish Health System in New York, who has conducted clinical trials of belimumab. "There's an awful lot of activity right now."

Lupus is a mysterious disease in which the immune system attacks healthy tissues. Nearly all lupus patients experience some degree of joint pain, and some will face life-threatening complications including kidney failure, heart problems and difficulty in breathing.

Belimumab is an antibody that interferes with the immune system's assault by binding to and inhibiting a protein called the 'B-lymphocyte stimulator' (BLyS). Blocking BLyS is thought to cause the immune system's antibody-producing B cells to self-destruct, thereby reducing the body's ability to attack its own tissues.

Belimumab was developed by Human Genome Sciences, a biotechnology company based in Rockville, Maryland, together with London-based pharmaceutical giant GlaxoSmithKline.(see more >>>)

Note:  Belimumab drug substance is a fully human IgG1λ monoclonal antibody. It has a typical antibody structure, composed of two identical H chains and two identical L chains, with a molecular weight of ~147 kDa. that belongs to the tumor necrosis factor (TNF) ligand family. 

    Copyright 2010 Chirosolve, Inc. All rights reserved.                                                            Vol2, Issue July 2011 Newsletter

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