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Medicilon assists Shijiazhuang No.4 Pharmaceutical's Class 1 new chemical drug SYN045 tablets obtain clinical approval

  On January 26, SYN045, a Class I new drug developed by Shijiazhuang No.4 Pharmaceutical, received a clinical trial approval notice from the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA).  This marks another substantial step forward in the research and development of the company's second innovative drug. Shanghai Medicilon Inc. (Medicilon), as a partner of Shijiazhuang No.4 Pharmaceutical, provided preclinical research services such as pharmacokinetics and safety evaluation for the development of SYN045 tablets, helping to successfully obtain approval. SYN045 is a Class I new drug independently developed by Shijiazhuang No.4 Pharmaceutical.  SYN045 is a selective long-acting PGI2 receptor agonist and is intended to be used for pulmonary arterial hypertension.  Preclinical studies have shown that SYN045 has good target selectivity, compound activity, and safety. Currently, Medicilon's preclinical research service platform has...

A Nickel-Catalyzed Reductive Alkylation of Aryl Bromides and Chlorides for Sp3-Sp2 Bond Formation

  In 2012, a nickel-catalyzed reductive alkylation method of aryl bromides and chlorides was reported. Under the optimized conditions, a variety of aryl and vinyl bromides as well as active aryl chloride can be reductively coupled with alkyl bromides in high yields. The protocols were highly functional-group tolerant and the reactions were not air or moisture sensitive. The reaction showed different chemoselectivity than conventional cross-coupling reactions. Substrates bearing both anelectrophilic and nucleophilic carbon resulted in selective coupling at the electrophilic carbon (R-X) and no reaction occurred at the nucleophilic carbon (R-[M]). The 2010 Nobel Prize in Chemistry was awarded for the Pd-catalyzed cross-coupling, and in the past decade the progress in cross-coupling has not only had a significant impact on academic research but has also influenced the industrial synthetic application. The transition-metal-catalyzed union of nucleophilic organo-boronic acids with elect...

Medicilon's Custom Peptide Synthesis Services

  Medicilon offers   custom synthetic peptides services   with a wide range of scales, purity levels, modifications and labeling, which allow you to get the highest performance in your research. Through our manufacturing and development of   peptides , we strive to provide a range of unique services that are not only high quality, but beneficial for our customers such as in the development of antibodies, substrates and probing protein-protein interactions. Our   synthesis services   are cost effective through our efficiency and knowledge, ensuring only the highest quality available.          ❖      Medicilon’s Synthetic Chemistry Services Medicilon can undertake the synthesis of special reagents, intermediates and molecular fragments, preparation of standard products, synthesis design and preparation of impurities or metabolites, synthesis of stable isotope internal standards and synthesis of tritiated compounds. Rela...

Organic Chemistry Synthesis of Medicilon

  As a leading provider of   chemical synthesis services , we provide reference compounds, intermediates, drug candidates, impurities, metabolites, and other  small molecule   chemicals from milligram to kilogram level (including GMP quality). The chemistry synthesis service comes with weekly updates, final reports and ordered amounts of the compound under strict confidentiality. Final reports contain sufficient information for you to readily repeat the chemistry in house if needed. Medicilon has synthesized 10,000 individual compounds from gram kilogram quantities, and many compounds are synthesized with more than ten synthetic steps. The overall synthesis success rate is over 95%. Chemical Synthesis Service We utilize medical chemistry and computational chemistry to design and synthesize drug-like templates and libraries of compounds to increase our client’s compound collections. The annual capacity of library production is more than 100,000 compounds. We have succ...

Fischer Indole Synthesis Reaction

  In 1883, E. Fischer and F. Jourdan treated pyruvate with 1-methylphenylhydrazone with HCl alcohol solution to obtain 1-methylindole-2-carboxylic acid. After this discovery, the Fischer indole synthesis reaction became a very significant method for the synthesis of substituted indoles. The Fischer indole synthesis reaction is a simple and rapid synthesis method for arylhydrazones obtained from the reaction of aldehydes or ketones with arylhydrazones.  The drug discovery of Medicilon mainly include chemistry (synthetic chemistry, medicinal chemistry) and biology. Among them, our chemistry team can undertake multi-dimensional business cooperation such as custom synthesis of compunds, compound library construction, SAR compound synthesis and screening, compound structure and biological activity optimization. This reaction is followed by cyclization to generate polysubstituted indoles. The phenylhydrazone generated in the reaction is heated and rearranged under acid catalysi...

What are chemically synthesized drugs? What are the synthetic methods of chemically synthesized drugs?

 Many people are curious about chemically synthesized drugs. In fact, in our lives, most of them are chemically synthesized drugs. The common ones are aspirin (acetylsalicylic acid), phenacetin, benzocaine, compound methoxy Naming and others. So how are they produced? The production methods of chemically synthesized drugs include total chemical synthesis, semi-synthesis, and chemical synthesis combined with microbial (enzyme-catalyzed) synthesis. What are the specific chemically synthesized drugs and what are the production methods of chemically synthesized drugs? Take a look at the article! 1. What are chemically synthesized drugs ? Chemically synthesized drugs refer to chemically synthesized drugs that are researched and produced according to chemical laws under the guidance of chemical theory. Generally speaking, it has a quick curative effect and a clear effect on disease treatment. The human body is a complex system, and chemically synthesized drugs lack the analysis and ...

Chiral Drug Synthesis

  Chiral drugs   refer to drugs that contain chiral centers (including chiral carbon, chiral nitrogen, chiral sulfur, etc.) in their molecular structure. In January 1992, the FDA promulgated the “Development of Stereoisomer Drugs” technical research guidelines, giving guidance on the work that needs to be done in the research of stereoisomer drugs. In December 2006, the CFDA issued the “Technical Guidelines for the Quality Control of Chiral Drugs”, which provided detailed guidance on the research work that needs to be carried out in the   synthesis process , structural confirmation and quality control research of chiral drugs, and indicated for the research of chiral drugs. Up the direction. As a special kind of chemical drugs, chiral drugs should not only follow the “Guiding Principles for the Research of Chemical Drug Preparation Processes”, but also combine the introduction of chiral centers to establish appropriate process control indicators for monitoring. The config...

Beautiful Chemistry-Photoinduced Alkene Cleavage Using Nitroarenes

  The oxidative cleavage of olefins is an important transformation in organic synthesis to obtain carbonyl functional groups such as ketones and aldehydes. The current used approaches, such as ozonolysis and Lemieux-Johnson Oxidation suffer from many significant limitations. Thus the development of a mild, general, and practical approach is still highly warranted. Oxidative Cleavage of Alkenes [1] A recent report from Parasram group (J. Am. Chem. Soc. 2022, 144, 15437.) indicated a visible light-induced anaerobic cleavage of alkenes by using economical and bench-stable nitroarenes as oxygen transfer reagents. The authors used 4-fluorostyrene as the control olefin to optimize the reaction conditions. They found 4-CN-nitrobenzene was the best nitroarene for such transformations. A few other nitroarenes bearing strong electron-withdrawing group gave satisfactory results, while nitroarene bearing electron-donating group gave poor conversion. Optimization of reaction condition [1] By us...