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Dive into the research topics where Thomas Nicola is active.

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Featured researches published by Thomas Nicola.


Organic Letters | 2010

Efficient Synthesis of a Small Molecule, Nonpeptide Inhibitor of LFA-1

Xiao-Jun Wang; Yibo Xu; Li Zhang; Dhileepkumar Krishnamurthy; Thomas Wirth; Thomas Nicola; Chris H. Senanayake

A three-stage process for the synthesis of LFA-1 inhibitor 1 from amine 4 with an overall yield of 65% is described. The key stage involves a Ph(3)PCl(2)-induced dehydration/cyclization of urea 6 followed by a regioselective bromination to give 1H-imidazo[1,2-a]imidazol-2-one 9. Br/Mg exchange of 9 followed by addition to SO(2) in THF and subsequent oxidation produces a sulfonyl chloride which is directly reacted with L-alaninamide using K(2)CO(3) as base in aqueous DMF/THF to give 1 in a one-pot operation. The process was implemented for the production of 1 on a metric ton scale.


Journal of Organic Chemistry | 2006

Efficient Large-Scale Synthesis of BILN 2061, a Potent HCV Protease Inhibitor, by a Convergent Approach Based on Ring-Closing Metathesis

Nathan K. Yee; Vittorio Farina; Ioannis N. Houpis; Nizar Haddad; Rogelio P. Frutos; Fabrice Gallou; Xiao-Jun Wang; Xudong Wei; Robert D. Simpson; XuWu Feng; Victor Fuchs; Yibo Xu; Jonathan Tan; Li Zhang; Jinghua Xu; Lana L. Smith-Keenan; Jana Vitous; Michael D. Ridges; and Earl M. Spinelli; Michael E. Johnson; Kai Donsbach; Thomas Nicola; Michael Brenner; Eric Winter; and Paul Kreye; Wendelin Samstag


Organic Process Research & Development | 2005

First Scale-Up to Production Scale of a Ring Closing Metathesis Reaction Forming a 15-Membered Macrocycle as a Precursor of an Active Pharmaceutical Ingredient

Thomas Nicola; Michael Brenner; and Kai Donsbach; Paul Kreye


Archive | 2005

Method for producing chiral 8-(3-amino-piperidin-1-yl)-xanthines

Waldemar Pfrengle; Thorsten Pachur; Thomas Nicola; Adil Duran


Archive | 2009

Process for the preparation of chiral 8-(3-aminopiperidin-1-yl)-xanthines

Waldemar Pfrengle; Thorsten Pachur; Thomas Nicola; Adil Duran


Archive | 2005

Process for continuous ruthenium-catalysed metathesis

Thomas Herweck; Albrecht Jacobi; Thomas Nicola; Michael Wiese


Archive | 2005

Verfahren zur herstellung chiraler 8-(3-amino-piperidin-1-yl)-xanthine

Waldemar Pfrengle; Thorsten Pachur; Thomas Nicola; Adil Duran


Archive | 2005

Process of removing transition metals

Michael Brenner; Kai Donsbach; Thomas Nicola; Thomas Wirth


Archive | 2005

Continuous metathesis method with ruthenium catalysts

Thomas Herweck; Albrecht Jacobi; Thomas Nicola; Michael Wiese


Archive | 2005

Method of removing transition metals from reaction solutions comprising transition metal byproducts

Michael Brenner; Kai Donsbach; Thomas Nicola; Thomas Wirth

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