AxisPharm’s Post

DOTA PEG https://lnkd.in/gj4QuzGX DOTA PEG linkers are an important class of molecules widely used in pharmaceutical research and development. These linkers are composed of a DOTA chelator and a polyethylene glycol (PEG) chain. The DOTA moiety is used to bind to metal ions such as copper, gallium or lutetium, while the PEG chain provides stability and solubility to the resulting conjugate.

Metal-free synthesis of heterocycles is highly sought after in the pharmaceutical industry and more so when the heterocycle happens to be a "Pyridine" ring. A new method reports a radical 6-endo addition method for pyridine synthesis from cyclopropylamides and alkynes wherein various terminal and substituted alkynes can be inserted as C2 units into cyclopropylamides to synthesize versatile pyridines to suit the late-stage pyridine installation on complex molecules. The reaction is amenable to easily scale up with excellent functional group compatibility while avoiding the headache of eliminating the need to remove trace metal catalysts from the reaction. https://lnkd.in/gBYvDQex

✅ Bicyclo[1.1.1]pentane (BCP) is a bridging ring skeleton with three-dimensional structure. ✅ BCP is a bioisostere of the phenyl ring, tert-butyl group, and alkynes; it has excellent physical and chemical properties compared with phenyl ring, so it has been widely considered by the pharmaceutical chemistry. ✍ This short review by Zhuohan Fang, Qian Xu, Xuehe Lu, Nianfeng Wang and Wu-Lin Yang considers the reports of BCP as a bioisostere of the phenyl ring, and the changes in physicochemical properties and biological activity after substitution.    👀 Read it here: https://lnkd.in/e347ebZE

There has always been a dearth of practical and efficient methods for accessing organic nitrates, which are quite famous in the pharmaceutical industry as effective donors of the signaling molecule nitric oxide, exemplified by well-known drugs such as glycerol trinitrate and isosorbide mononitrate. A new study reports practical and regioselective halonitrooxylation of a wide variety of unactivated olefins to access β-halonitrates. The protocol offers high efficiency, mild conditions, simple operation, and good compatibility with various functional groups. Especially, the product of ethylene iodonitrooxylation, 2-iodoethyl nitrate, can be combined with a range of natural products and drugs to obtain corresponding nitrooxylated functional molecules. The potential utility of the method is further highlighted by the gram-scale preparation and late-stage modification of bioactive molecules. https://lnkd.in/gYPNw-fj

Magnesium Carbonate is an inorganic compound with the chemical formula MgCO3. Magnesium Carbonate is a common antacid drug that is used Pharmaceutical Aid; Magnesium Carbonate contains not less than 40.0 per cent and Not more than 45.0 per cent of MgO. https://buff.ly/3JYiddJ #MagnesiumOxide #MagnesiumCarbonate #Foodadditives #CosmeticManufacturing #MagnesiumSulfate #MagnesiumHydroxide

Harnessing strain-release driven reactivity of a chiral SuFEx reagent: Stereocontrolled access to sulfinamides, sulfonimidamides, and sulfoximines. The amine exchange can be done at either the S(IV) or S(VI) oxidation state, leading to diverse chemical space suitable for pharmaceuticals and organocatalysts. Over 70 examples highlight the broad functional group tolerance with an emphasis on complex pharmaceutical amines. Highly functionalized sulfonimidoyl ureas from a common precursor. https://lnkd.in/gfRKY-cz

𝗕𝗼𝗿𝗼𝗻-𝗖𝗼𝗻𝘁𝗮𝗶𝗻𝗶𝗻𝗴 𝗕𝘂𝗶𝗹𝗱𝗶𝗻𝗴 𝗕𝗹𝗼𝗰𝗸𝘀 𝗳𝗼𝗿 𝗠𝗲𝗱𝗶𝗰𝗶𝗻𝗮𝗹 𝗥𝗲𝘀𝗲𝗮𝗿𝗰𝗵: 𝗕𝗲𝗻𝘇𝗼𝘅𝗮𝗯𝗼𝗿𝗼𝗹𝗲𝘀 Boronic acids are recognized as useful scaffolds for pharmaceutical compounds, due to their unique property to form a reversible covalent bond at the boron center with various nucleophilic functional groups. TCI can offer a wide range of benzoxaboroles with various functional groups on each benzene ring useful for further derivatizations and we also can provide custom synthesis of derivatives including bulk synthesis. 𝗟𝗲𝗮𝗿𝗻 𝗠𝗼𝗿𝗲: https://lnkd.in/gSfn7tGK #bulksynthesis #customsynthesis #pharmaceuticalcompounds #benzoxaboroles #medicinalresearch #boronicacids #researchchemicals #reagents

Suzuki–Miyaura cross-coupling (SMC) is widely used in the pharmaceutical industry to form carbon-carbon bonds but traditionally requires a base, which limits its substrate compatibility. Many boronic acids and Lewis-basic functional groups can't be used due to instability or catalyst poisoning. The new approach described allows SMC to proceed under acidic conditions, avoiding the need for a base. This is achieved by forming an acid-stable palladium-based ion pair, enabling the use of boronic acids, such as 2-pyridylboronic acid, that were previously incompatible with standard methods, thus expanding the reaction's substrate scope. https://lnkd.in/dZy6wDSt

2-Methyltetrahydrofuran(CAS No.:96-47-9) 👆 👆 👆 👆 👆 USEs: 1. as solvent, such as used in Grignard Reaction. 2. Used in automotive fuel additive 3. as solvents for resin, rubber, ethyl cellulose 4. used for Anti-disease drugs synthesis, such as primaquine phosphate and chloroquine phosphate in the pharmaceutical industry