Showing papers in "Organic Process Research & Development in 2011"

TL;DR: The American Chemical Society Green Chemistry Institute's Pharmaceutical Roundtable has chosen process mass intensity (PMI) as the key, high-level metric for evaluating and benchmarking progress towards more sustainable manufacturing as mentioned in this paper.

TL;DR: It is seen that the fermentation yield in terms of final achievable cell concentration and expression level as well as the production scale are crucial for decreasing the total cost contribution of the biocatalyst.

TL;DR: The American Chemical Society (ACS) Green Chemistry Institute (GCI) and global pharmaceutical companies established the ACS GCI Pharmaceutical Roundtable to encourage the integration of green chemistry and engineering into the pharmaceutical industry as mentioned in this paper.

TL;DR: The immobilization of enzymes as cross-linked enzyme aggregates (CLEAs) and their applications in industrially relevant biotransformations are reviewed and co-aggregation and cross-linking of ...

TL;DR: A brief account highlights the remarkable versatility of dirhodium-based catalysts for promoting oxidation of aliphatic C-H centers in both intra- and intermolecular reaction processes.

TL;DR: Enzymes are an important part of industry due to their many favorable properties and have found use in many industries including food, detergents, textiles, leather, pulp and paper, diagnostics, and therapy.

TL;DR: Evaluation of the oral toxicity of MeTHF and CPME as determined in three month repeat-dose toxicity studies in rats as well as a battery of tests conducted under Good Laboratory Practice (GLP) to assess induction of micronuclei, microbial mutagenicity, and chromosomal aberrations.

TL;DR: In this review, a classification of multienzyme-catalyzed processes is proposed, special emphasis is placed on the description ofMultienzyme ex-vivo systems where several reactions are carried out by a combination of enzymes acting outside the cell.

TL;DR: In this paper, an automated, silicon microreactor system that uses a sequential experimentation framework driven by model-based optimization feedback for online reaction rate parameter determination is presented, based on Information Theory and Bayesian Statistics.

TL;DR: In this article, a commercial agitating cell reactor which uses a transverse mixing motion to maintain solids in suspension has been successfully applied to a salt-forming reaction, delivering 208 g of N-iodomorpholinium hydroiodide salt over a 9-h period (equating to 3.88 kg/week).

TL;DR: In this paper, a series of different monomers, including acrylamides, acrylates, and vinyl acetate, were polymerized to high conversions at temperatures between 70 and 100 °C using various initiators, solvents, and RAFT agents.

TL;DR: A new synthetic route to drug candidate 1, a potent and selective dual orexin antagonist for the treatment of sleep disorders, has been developed using novel chemistry to synthesize 2-substituted benzoxazoles.

TL;DR: Hydrogenation of π-unsaturated reactants in the presence of carbonyl compounds or imines promotes reductive C-C coupling, providing a byproduct-free alternative to stoichiometric organometallic reagents in an ever-increasing range of C=X (X = O, NR) additions.

TL;DR: A robust six-step process for the synthesis of crizotinib, a novel c-Met/ALK inhibitor currently in phase III clinical trials, has been developed and used to deliver over 100 kg of API as mentioned in this paper.

TL;DR: The first kilogram-scale application of this technology in the synthesis of PF-03463275, a GlyT1 inhibitor developed for the treatment of schizophrenia, was described in this article.

TL;DR: In this article, a continuous flow microreactor is applied for a kinetic study of a model β-amino alcohol formation by epoxide aminolysis, and a large number of experiments are performed in a short time with minimal reagent consumption.

TL;DR: In this paper, the use of flow chemistry for scaling up exothermic or hazardous nitration reactions was described, including a reaction involving a potentially explosive mixture of acetic acid and fuming nitric acid, with a productivity of 97 g/h.

TL;DR: This contribution gives an overview of the different strategies to increase the final titer, yield, and productivity of 1,3-propanediol in non-natural and natural producing strains.

TL;DR: An immobilized form of Candida antarctica lipase B (CAL-B) has been developed with enhanced stability and activity compared to commercially available preparations, which permits a continuous dynamic kinetic resolution process that is significantly less expensive than the original batch process, and with a 3-fold reduction in the process E-factor.

TL;DR: Three different continuous flow strategies for the generation of important 4-aryl-2-butanone derivatives including the anti-inflammatory drug nabumetone [4-(6-methoxy)-2-naphthalenyl)-2-(2.

TL;DR: In this article, the development of a second-generation process for the synthesis of eletriptan via a Fischer indole cyclisation is described, which offers several potential advantages over the current route of manufacture including cost, throughput, and safety.

TL;DR: In this article, a self-optimizing continuous flow reactor was developed using the Super-Modified Simplex algorithm, which combined with online gas chromatographic analysis enables automated optimization.

TL;DR: In this paper, an evaluation of a new bench-top microwave batch reactor that uses a single 1 L reaction vessel is presented, and isolated product yields up to 300 g (2.5 mol scale) in a single run could be achieved, providing the po...

TL;DR: In this article, the FBRM probe is used to investigate a crystallization of needle-shaped particles to develop a crystallisation that can deliver product within the required quality attributes.

TL;DR: The commercial potential of biotechnology is huge, a colossal 1000 billion U.S. dollars, or about an order of magnitude more than today! in order not to disappoint investors and tax payers, however, the authors need to develop their tools further, especially for complex molecules for various applications.

TL;DR: In this article, a high efficient and environmentally friendly procedure for the production of aromatic and heteroaromatic β-nitroalcohols has been developed, which involves the condensation of an...

TL;DR: A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key, highly functionalized hydroxypyrimidin this paper.

TL;DR: A flow chemistry method for the synthesis of pyrroles was developed, optimized in 0.13 to 7 μL microreactors in continuous flow, reaching yields of nearly 100%, leading to production of a pyrrole derivative at a rate of 55.8 g per hour.

TL;DR: The synthetic route to AMG 837 involved the convergent synthesis and coupling of two key fragments, (S)-3-(4-hydroxyphenyl)hex-4-ynoic acid (1) and 3-(bromomethyl)-4′-(trifluorometHyl)biphenyl (2), and a sodium salt form was selected for early development and salt selection.