Showing papers in "Organic Process Research & Development in 2019"

TL;DR: This review will deliver an overview of the latest best practices currently taking place within teams in process chemistry by sharing frequently studied transformations, the perspective for the next several years in the field, and manual and automated tools to enable experimentation.

TL;DR: This review will discuss several recent examples of continuous biotransformations that use immobilization, with a focus on examples involving fine chemical synthesis and some of the issues the community has as a whole.

TL;DR: The palladium-catalyzed cross-coupling of amines and aryl (pseudo)halides, now commonly known as the Buchwald-Hartwig amination, was first reported 25 years ago as discussed by the authors.

TL;DR: Continuous crystallization has gained interest in the pharmaceutical sector as part of the drive toward the transition from exclusive batch manufacturing to integrated continuous manufacturing in this industry as mentioned in this paper, as a result, the design and operation of continuous crystallization processes for the preparation of pharmaceutical materials has been featured strongly in recent scientific literature.

TL;DR: This review presents the Analytical quality by Design concept, an extension of Quality by Design (QbD), which was introduced in 2004 by the U.S. Food and Drug Administration (FDA) and approv...

TL;DR: The hazards associated with the thermal decomposition of chemically incompatible sodium hydride solvent matrices are known, with reports from the 1960s detailing the inherent instability of NaH/dimethyl sulfoxide and N-dimethylformamide mixtures as mentioned in this paper.

TL;DR: While reductive cross-electrochemical coupling is an attractive approach for the synthesis of complex molecules at both small and large scale, two barriers for large scale applications have remaine... as discussed by the authors.

TL;DR: In this paper, a detailed exploration of cycloadditions, in flow, of various maleic anhydride derivatives with gaseous ethylene was carried out by the use of a flow reactor capable of gas handling and LED wavelength/power screening.

TL;DR: In an undivided multichannel electrochemical flow reactor at ambient temperature and pressure in basic reaction conditions, the yield of furfuryl alcohol reached up to 90% in only 10 min residence time, showing a good effectiveness of the consumed electrons in the generation of the targeted compound.

TL;DR: The first non-phosgene polycarbonate process from CO2 has been developed and industrialized by Asahi Kasei Corporation (Japan) as mentioned in this paper, where high-quality polycarbonates and high-purity monoethylene glycol (MEG) are produced in high yields, respectively, without waste and wastewater, starting from CO 2, ethylene oxide (EO), and bisphenol A (BPA).

TL;DR: This research presents a novel, scalable, and scalable approaches that allow for real-time measurement of the response time of visible-light photoredox reactions to investigate the chiral stationary phase of these reactions.

TL;DR: In this paper, Pd-catalyzed carbon-nitrogen cross-coupling has enabled the use of soluble organic bases instead of insoluble or strong inorganic bases that are traditionally employed.

TL;DR: The widespread use of amidine and guanidine bases in synthetic chemistry merits a thorough understanding of their chemical properties and the propensity of these reagents to hydrolyze under mild condi....

TL;DR: In this article, an efficient synthetic route for an optically active ceramide compound (d-erythro-CER[NDS]) is described, which proceeds through asymmetric transfer hydrogenation in a pipes-in-series flow reactor with oxo-tethered ruthenium complex-catalyzed dynamic kinetic resolution.

TL;DR: Development of a small volume continuous process that used a combination of batch and flow unit operations to manufacture the small molecule oncolytic candidate merestinib is described.

TL;DR: Desorption electrospray ionization mass spectrometry was used to quickly explore a large number of reaction conditions for one of the reaction steps and guide the efficient translation of optimized conditions to continuous lomustine production.

TL;DR: In this article, an aerobic oxidation reaction of alcohols toward aldehydes or ketones using catalytic amounts of Fe(NO3)3·9H2O, 4-OH-TEMPO, and NaCl has been developed.

TL;DR: In this article, the authors used ATR FTIR and an online imaging instrument with the aim of developing an improved understanding of the operation and condition optimization and scale-up of Cefixime trihydrate crystals.

TL;DR: In this paper, the catalytic activity of the pentamethylcyclopentadienylsilicon(II) cation Cp*Si:+ was investigated, and it was shown that it efficiently catalyzes reactions of technical relevance in organosilic...

TL;DR: The maximum solubilities of iridium and ruthenium centered photocatalysts have been systematically identified in industrially relevant solvents to make these reactions appear less efficient than they actually are.

TL;DR: Citronellal cyclization was carried out in a continuous mode over H-beta-25 zeolite-based extrudates in a trickle-bed reactor at 35 °C and 10 bar of Ar.

TL;DR: The feasibility of using tandem cage-walking/cross-coupling as a unique low-temperature method for producing regioisomers of mono-substituted carboranes by tuning the transmetallation step in the catalytic cycle is demonstrated.

TL;DR: A practical asymmetric synthesis of an enantiomerically 97.8% ee pure N-Fmoc derivative of (S)-2-amino-4,4, 4,4-trifluorobutanoic acid performed on >10 g scale of the target product is disclosed.

TL;DR: The tetrasubstituted pyrrolidine core of ABBV-3221 was synthesized by catalytic, enantioselective cycloaddition as discussed by the authors.

TL;DR: This work describes the evolution of the chemical processes, following the manufacture of AZD6738 from the initial scale-up through to multikilos on plant scale and discusses the impurities formed throughout the process.

TL;DR: In this article, the authors propose to use a high substrate concentration with high substrate diversity for the catalytic dehydration of C6 sugars, a product of catalytic de-watering.

TL;DR: Kinetic studies revealed that IRED-33 was the best enzyme for the reaction with respect to both activity and stability, and under the optimal reaction conditions, it was possible to react 1 and 2 at 750 mM concentration and reach 100% conversion to the desired amine in the space of 8 h.

TL;DR: A third inhibitor, cabotegravir, is in Phase 3 development, and a continuation of a series of series of approvals for integrase inhibitors for the treatment of HIV.

TL;DR: In this paper, a family of 6-hydroxypicolinamide ligands have been identified as effective supporting ligands for Cu-catalyzed couplings of heteroaryl bromides and chlorides with HPC amines.

TL;DR: In this article, a reactive seeded cooling crystallization of paracetamol successfully performed in a continuous oscillatory baffled reactor (COBR), enabling smooth and encrustation-free runs.