Improving the solubility of berberine

A possible solution for improving the water solubility of berberine by the formation of multicomponent pharmaceutical salts provides the background for this commentary.     

An alternative efficient approach for the synthesis of Fingolimod hydrochloride

An efficient process for the synthesis of API Fingolimod Hydrochloride is presented. This proposed synthesis involves simple commercially available octanophenone as a starting material. The route is effective involving seven steps to achieve the target, thus reducing the cycle time, and is cost efficient by 50%. It is an immune modulating drug for the treatment of heart failure and arrhythmias.     

Cavitation based cleaner technologies for biodiesel production and processing of hydrocarbon streams: A perspective on key fundamentals,missing process data and economic feasibility – A review

The present review emphasizes the role of hydrodynamic cavitation (HC) and acoustic cavitation in clean and green technologies for selected fuels (of hydrocarbon origins such as gasoline, naphtha, diesel, heavy oil, and crude oil) processing applications including biodiesel production. Herein, the role of cavitation reactors, their geometrical parameters, physicochemical properties of liquid media, liquid oxidants, catalyst loading, reactive oxygen species, and different types of emulsification and formation of radicals, formation as well as extraction of formed by-products are systematically reviewed. Among all types of HC reactors, vortex diode and single hole orifices revealed more than 95 % desulfurization yield and a 20 % viscosity reduction in heavy oil upgrading, while multi-hole orifice (100 holes) and slit Venturi allowed obtaining the best biodiesel production processes in terms of high (%) yield, low cost of treatment, and short processing time (5 min; 99 % biodiesel; 4.80 USD/m³). On the other hand, the acoustic cavitation devices are likely to be the most effective in biodiesel production based on ultrasonic bath (90 min; 95 %; 6.7 $/m³) and desulfurization treatment based on ultrasonic transducers (15 min; 98.3 % desulfurization; 10.8 $/m³). The implementation of HC-based processes reveals to be the most cost-effective method over acoustic cavitation-based devices. Finally, by reviewing the ongoing applications and development works, the limitations and challenges for further research are addressed emphasizing the cleaner production and guidelines for future scientists to assure obtaining comprehensive data useful for the research community.     

Supramolecular architectures in two 1:1 cocrystals of 5‐fluorouracil with 5‐bromothiophene‐2‐carboxylic acid and thiophene‐2‐carboxylic acid

In solid‐state engineering, cocrystallization is a strategy actively pursued for pharmaceuticals. Two 1:1 cocrystals of 5‐fluorouracil (5FU; systematic name: 5‐fluoro‐1,3‐dihydropyrimidine‐2,4‐dione), namely 5‐fluorouracil–5‐bromothiophene‐2‐carboxylic acid (1/1), C₅H₃BrO₂S·C₄H₃FN₂O₂, (I), and 5‐fluorouracil–thiophene‐2‐carboxylic acid (1/1), C₄H₃FN₂O₂·C₅H₄O₂S, (II), have been synthesized and characterized by single‐crystal X‐ray diffraction studies. In both cocrystals, carboxylic acid molecules are linked through an acid–acid R ₂²(8) homosynthon (O—H…O) to form a carboxylic acid dimer and 5FU molecules are connected through two types of base pairs [homosynthon, R ₂²(8) motif] via a pair of N—H…O hydrogen bonds. The crystal structures are further stabilized by C—H…O interactions in (II) and C—Br…O interactions in (I). In both crystal structures, π–π stacking and C—F…π interactions are also observed.     

荧光试剂3-(4-氨基苯基)中氮茚-1-羧酸甲酯用于亚硝酸根测定

介绍了一种新的测定亚硝酸根的荧光探针分子———3-(4-氨基苯基)中氮茚-1-羧酸甲酯(API)。API在酸性介质中与亚硝酸根生成重氮盐化合物,进一步在碱性介质中生成相应的羟基二氮烯,使荧光强度明显增强。基于该反应,提出了一种操作简便、灵敏度高、选择性好的亚硝酸根荧光测定方法。该方法对亚硝酸根检测的线性范围为4.5×10-8~7.5×10-6mol/L,检出限为8.3×10-9mol/L(0.38μg/L,S/N=3)。用于检测水体中亚硝酸根浓度,取得了满意的结果。     

A Concise Flow Synthesis of Efavirenz

Efavirenz is an essential medicine for the treatment of HIV, which is still inaccessible to millions of people worldwide. A novel, semi‐continuous process provides rac‐Efavirenz with an overall yield of 45 %. This streamlined proof‐of‐principle synthesis relies on the efficient copper‐catalyzed formation of an aryl isocyanate and a subsequent intramolecular cyclization to install the carbamate core of Efavirenz in one step. The three‐step method represents the shortest synthesis of this life‐saving drug to date.     

Mixed Ca/Sr salt forms of salicylic acid: tuning structure and aqueous solubility

Ten isostructural single‐crystal diffraction studies of mixed cation Ca/Sr salt forms of the salicylate anion are presented, namely catena‐poly[[diaquacalcium(II)/strontium(II)]‐bis(μ₂‐2‐hydroxybenzoato)], [Ca_1–xSr_x(C₇H₅O₃)₂(H₂O)₂]_n, where x = 0, 0.041, 0.083, 0.165, 0.306, 0.529, 0.632, 0.789, 0.835 and 1. The structure of an isostructural Sr/Ba species, namely catena‐poly[[diaquastrontium(II)/barium(II)]‐bis(μ₂‐2‐hydroxybenzoato)], [Sr_0.729Ba_0.271(C₇H₅O₃)₂(H₂O)₂], is also described. The Ca/Sr structures form a series where, with increasing Sr content, the unit cell expands in both the crystallographic a and c directions (by 1.80 and 3.18%, respectively), but contracts slightly in the b direction (−0.31%). The largest percentage structural expansion lies parallel to the direction of propagation of the one‐dimensional coordination polymer that is the primary structural feature. This structural expansion is thus associated with increased M—O distances. Aqueous solubility measurements show that solubility generally increases with increasing Sr content. Thus, tuning the composition of these mixed counter‐ion salt forms leads to systematic structural changes and allows solubility to be tuned to values between those for the pure Ca and Sr species.