Clopidogrel series drug intermediate production project introduction

I. Company Profile
　　Shanghai JIN DUN Industrial Co., Ltd was founded in 2013 and is located in Shanghai. With senior American scientists as the core and a team of internationally renowned experts as advisors, the company has gathered industry elites to lead the R&D innovation in medicinal chemistry, focusing on the technological development and industrialization of high-end generic drugs, high value-added drug intermediates, and new tumor diagnostic reagents.
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　　II. Clopidogrel series intermediates product introduction
　　Clopidogrel, Prasugrel and Ticlopidine are antithrombotic drugs. Clopidogrel is a super heavyweight drug, with global sales exceeding USD 10 billion in 2010. After the patent of clopidogrel expired in 2012, the market share further increased. Prasugrel and ticlopidine, both important complementary brands in the antithrombotic market, also have annual sales of more than $1 billion.
　　All three drugs are manufactured with 2-(2-Thienyl)ethanol (structure I), or 2-(2-Thienyl)ethylamine (structure II), or tetrahydrothieno[3,2-c]pyridine (structure III) as key ingredients. (structure III) as key ingredients.
　　The company has successfully developed a new production process for the above mentioned series of intermediates: 2-thiopheneethanol, 2-thiopheneethylamine and tetrahydrothieno[3,2-c]pyridine for this heavy drug market. Compared with the traditional process in the market, the new process has completely different raw materials, shorter process route, higher yield and lowest cost, and has absolute advantages over other production technologies, with good prospects for industrialization. The main features of the process route are:
　　(i) Lowest cost. After adopting the modified process, the production cost of the product is reduced by about 20% compared with the traditional process, and the gross margin of the product can reach 40%.
　　(2) Excellent quality. The product "2-thiopheneethanol" produced by the modified process does not contain the key isomeric impurity "3-thiopheneethanol", which is inevitably produced by the traditional process, and the quality is significantly improved.
　　(3) Less pressure on environmental protection. Under the pressure of the new environmental protection policy, the environmental pressure on the industrialization of the new process is minimal.
　　(iv) The process is mature and feasible. At present, this type of process has been verified by the plant scaling up production (110kg at one feeding), and the process is mature and stable.
　　At present, the domestic core suppliers of this series of intermediates are mainly one enterprise each in Zhejiang and Shandong. Due to the influence of traditional process and environmental protection policy, Shandong enterprises have basically stopped the production of this series of products, the market is in short supply, the current market price of "2-thiopheneethanol" is about 110,000 yuan / ton, the price is expected to go up.
　　III. Other generic drug projects
　　At present, the company has completed the following generic drug process technology research, if interested, we can discuss cooperation or technology transfer.
　　1、The synthesis process and quality research of moxifloxacin, a super broad-spectrum antibacterial fluoroquinolone drug.
　　2, Synthesis process and quality research of non-addictive analgesic flupirtine maleate.
　　3, process development and quality study of esomeprazole sodium, an efficient and safe anti-gastrointestinal ulcer drug.
　　4, synthesis process and quality study of safe and efficient sedative-hypnotic agent phosphoprotol sodium.
　　5. Synthesis process and quality study of prasugrel hydrochloride for the treatment of angina pectoris and coronary syndrome.
　　6、Synthesis process and quality study of ceftazidime, a semi-synthetic broad-spectrum antimicrobial agent.
　　7、Synthetic process of lipid-lowering drug Clifedet.
　　8, Synthesis process of tolvaptan, the drug of choice for the treatment of low blood sodium.
　　9, Synthesis process of the drug Rexagiline for the treatment of Parkinson's disease.
2-bromo-2-(2-fluorophenyl)-1-cyclopropylethanone is used as the intermediate of Prasugrel.
Prasugrel is a thiophenopyridine antiplatelet developed by Eli Lilly and daiichisankyo, a Japanese pharmaceutical manufacturer. It is a precursor drug. It forms an active molecule after metabolism through cytochrome P450 in the liver and combines with platelet P2Y12 receptor to exert an active against platelet aggregation. Clinical studies have proved that 60 mg dose has better anticoagulant effect than 300 mg standard dose and 600 mg increased dose of clopidogrel, which can reduce the comprehensive risk of heart attack, stroke and death due to heart disease by 20%, and has fast effect, good curative effect, good drug resistance and bioavailability, and low toxicity.