Алгоритм расчета необходимого продовольственного потенциала региона и его реализация

У роботі викладено необхідність розробки стратегії забезпечення населення продовольством на основі аналізу сучасного економічного стану сільськогосподарського виробництва та випуску продукції в регіоні.The need for the strategy of the population provision with food considering modern economic situation with agricultural production is shown. Analysis of food production in the region is conducted

Stereoselective Synthesis of (<i>S</i>)-3-(Methylamino)-3-((<i>R</i>)-pyrrolidin-3-yl)propanenitrile

(<i>S</i>)-3-(Methylamino)-3-((<i>R</i>)-pyrrolidin-3-yl)­propanenitrile (<b>1</b>) is a key intermediate in the preparation of PF-00951966, a fluoroquinolone antibiotic for use against key pathogens causing community-acquired respiratory tract infections including multidrug resistant (MDR) organisms. The current work describes the development of a highly efficient and stereoselective synthesis of <b>1</b> in 10 steps with an overall yield of 24% from readily available benzyloxyacetyl chloride. Two key transformations in the synthetic sequence involve (a) catalytic asymmetric hydrogenation with chiral DM-SEGPHOS-Ru­(II) complex to afford β-hydroxy amide <b>11b</b> in good yield (73%) and high stereoselectivity (de 98%, ee >99%) after recrystallization and (b) S_N2 substitution reaction with methylamine to provide diamine <b>14</b> with inversion of configuration at the 1′-position in high yield (80%), after efficient purification using a simple acid/base extraction protocol

Early Process Development of Two Vanin‑1 Inhibitors: Solid Form Challenges and Control of Ambident Reactivity

Discovery chemistry efforts within Pfizer identified a new vanin-1 inhibitor, (S)-1, bearing a chiral methyl substituent, which exhibited an excellent profile as a potential drug-candidate selection except for the propensity to exist as an amorphous solid. Based on an improved solid form proposition, the project team chose to prioritize 2, the corresponding des-methyl compound. Both compounds were scaled to supply toxicology studies in preclinical species, and kilograms of compound 2 were manufactured to support the preclinical development work. The development of our synthetic chemistry and solid form work on this program are described in the paper. Included are computational studies to rationalize both an expected TBD-mediated epimerization as well as the control of ambident reactivity of activated 2-chloro-pyrimidine-5-carboxylic acid

Process Development for the Synthesis of Monocyclic β‑Lactam Core 17

Process development and multikilogram synthesis of the monocyclic β-lactam core <b>17</b> for a novel pyridone-conjugated monobactam antibiotic is described. Starting with commercially available 2-(2,2-diethoxyethyl)­isoindoline-1,3-dione, the five-step synthesis features several telescoped operations and direct isolations to provide significant improvement in throughput and reduced solvent usage over initial scale-up campaigns. A particular highlight in this effort includes the development of an efficient Staudinger ketene–imine [2 + 2] cycloaddition reaction of <i>N</i>-Boc-glycine ketene <b>12</b> and imine <b>9</b> to form racemic β-lactam <b>13</b> in good isolated yield (66%) and purity (97%). Another key feature in the synthesis involves a classical resolution of racemic amine <b>15</b> to afford single enantiomer salt <b>17</b> in excellent isolated yield (45%) with high enantiomeric excess (98%)