Innovation in API Synthesis

Van Arnum, Patricia
February 2007
Pharmaceutical Technology;Feb2007, Vol. 31 Issue 2, p50
Trade Publication
The article reports that custom manufacturers are challenged by pharmaceutical industries to manufacture increasingly complex molecules with cost-effective routes. Degussa GmbH has taken a route to synthesize an enantiomerically pure aminolactam, a chiral building block for a new antithrombotic. BioCatalytics Inc. has developed a range of ketoreductases for the stereoselective reduction of ketones. Also, other companies are advancing biocatalysis for API synthesis.


Related Articles

  • Achieving Enantioselectivity in Synthesizing APIs and Intermediates. van Arnum, Patrician // Pharmaceutical Technology;Oct2006 CPhl Supplement, Vol. 30, ps20 

    The article reports on the importance of biocatalysis and chemocatalysis in asymmetric reactions used by custom manufacturers and technology providers. David Rozzell, president and CEO of BioCatalytics Inc. said that after chemists ignored biocatalysis, it became increasingly important in...

  • Biocatalysis: Synthesis of Chiral Intermediates for Pharmaceuticals. Patel, Ramesh N. // Current Organic Chemistry;Jul2006, Vol. 10 Issue 11, p1289 

    The production of single enantiomers of drug intermediates has become increasingly important in the pharmaceutical industry. Chiral intermediates and fine chemicals are in high demand by both the pharmaceutical and agrochemical industries for the preparation of bulk drug substances and...

  • Synthesis, Chiral Separation, Barrier to Rotation and Absolute Configuration of N-(O- Functionalized-Aryl)-4-Alkyl-Thiazolin-2-One and Thiazoline-2-Thione Atropisomers. Vanthuyne, Nicolas; Andreoli, Federico; Fernandez, Sylvie; Roman, Mihaela; Roussel, Christian // Letters in Organic Chemistry;Aug2005, Vol. 2 Issue 5, p433 

    The synthesis of N-(o-aryl)-4-alkyl-thiazolin-2-one atropisomers bearing hydroxy-, methoxy-, amino- or isothiocyanato- groups as ortho-substituent are described from their thiazoline-2-thione analogues. The enantiomers were obtained optically pure by semi-preparative chiral HPLC, their optical...

  • Building Toolboxes in Pursuit of Single-Enantiomer Drugs. Van Arnum, Patricia // Pharmaceutical Technology;Sep2011, Vol. 35 Issue 9, p54 

    The article focuses on the building of toolboxes in quest of single-enantiomer drugs in the U.S. It discusses how the strengthening capabilities in biocatalysis, chemocatalysis and other chiral technologies continue to attract the investment of fine-chemical companies and technology providers in...

  • CHEMOENZYMATIC DYNAMIC KINETIC RESOLUTION AS A KEY STEP IN THE ENANTIOSELECTIVE SYNTHESIS OF (S)-SALBUTAMOL. Träff, Annika; Solarte, Carmen E.; Bäckvall, Jan-E. // Collection of Czechoslovak Chemical Communications;2011, Vol. 76 Issue 7, p919 

    The synthesis of (S)-salbutamol is described. By utilizing DKR in the enantiodetermining step, employing Burkholderia cepacia lipase (PS-IM), (S)-acetate ((S)-6) was obtained in excellent enantiomeric excess (98%). The subsequent transformations yielded the salt of (S)-salbutamol with retained...

  • Asymmetric Synthesis of α-Aminophosphonates Using the Inexpensive Chiral Catalyst 1,1′-Binaphthol Phosphate. Weiming Xu; Sha Zhang; Song Yang; Lin-Hong Jin; Bhadury, Pinaki S.; De-Yu Hu; Yuping Zhang // Molecules;Aug2010, Vol. 15 Issue 8, p5782 

    Asymmetric addition under mild conditions of dialkyl phosphites on aldimines derived from cinnamaldehyde catalyzed by the inexpensive chiral organocatalyst (R)-3,3'- [4-fluorophenyl]2-1,1'-binaphthol phosphate has been found effective to give new α- amino-phosphonates 9 in moderate yields...

  • Recent Advances in Catalytic Asymmetric Addition to Imines and Related C=N Systems. Vilaivan, Tirayut; Bhanthumnavin, Worawan; Sritana-Anant, Yongsak // Current Organic Chemistry;Sep2005, Vol. 9 Issue 14, p1315 

    Addition reactions to imines are relatively less developed compared to those of carbonyl compounds due to low electrophilicity and ease of a-deprotonation. With the use of an appropriate activator, which can coordinate to the imine nitrogen atom, the electrophilicity of the imine can be enhanced...

  • Asymmetric oxidation of 4-nitro-6-trifluoromethyl-1,2,3-benzotrithiole. Khomenko, T.; Korchagina, D.; Volcho, K.; Salakhutdinov, N. // Russian Journal of Organic Chemistry;Sep2009, Vol. 45 Issue 9, p1402 

    Both enantiomers of 4-nitro-6-trifluoromethyl-1,2,3-benzotrithiole 1-oxide as analogs of Varacins B and C were synthesized for the first time. The use of the Modena method ensures higher optical purity but lower yields of the chiral sulfoxides, as compared to the Kagan procedure.

  • Features and technical applications of ω-transaminases. Malik, M.; Park, Eul-Soo; Shin, Jong-Shik // Applied Microbiology & Biotechnology;Jun2012, Vol. 94 Issue 5, p1163 

    Chiral amines in enantiopure forms are important chemical building blocks, which are most well recognized in the pharmaceutical industries for imparting desirable biological activity to chemical entities. A number of synthetic strategies to produce chiral amines via biocatalytic as well as...


Read the Article


Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics