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项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点:源头优选:利用如N-硝胺化学等底层方法学突破,从分子层面颠覆传统高成本、高污染路线。过程强化:依托连续流技术,攻克有机金属试剂应用、光化学反应放大等“不可能”任务,实现高危工艺的本质安全。系统集成:整合“反应-淬灭-分离”全流程,利用微流控与在线分析技术,消除批次间的差异,实现药品制造的连续化与智能化。当前,中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合,将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势,将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

  • Iminodisuccinic Acid CAS Registry Number: 7408-20-0; 70543-06-5 (stereo unspecified) L-天冬氨酸,N-(1,2-二羧乙基)-


    CAS Name: N-[(1S)-1,2-Dicarboxyethyl]-L-aspartic acid
    Additional Names: 2,2'-iminodisuccinic acid
    Percent Composition: C 38.56%, H 4.45%, N 5.62%, O 51.37%
    Literature References: Synthesis of ester from fumaric acid, ammonia and water: G. Stadnikoff, Ber. 44, 44 (1911). Industrial processes: GB 1306331 (1971 to Pfizer); T. Groth et al., US 6107518 (2000 to Bayer). Synthesis and complex forming properties: E. D. Malakhaev et al., J. Gen. Chem. USSR 48, 2361 (1978). Thermochemical study: V. P. Vasil'ev et al., Russ. J. Phys. Chem. 63, 1566 (1989). Formation constants with metal cations: C. K. Gangoda, D. R. Williams, Chem. Speciation Bioavailab. 9, 101 (1997).

  • Methioprim CAS Registry Number: 588-36-3 2-甲硫基-4-氨基嘧啶-5-甲醇


    CAS Name: 4-Amino-2-methylthio-5-pyrimidinemethanol
    Additional Names: 4-amino-2-methylmercapto-5-pyrimidinemethanol; 4-amino-5-hydroxymethyl-2-methylthiopyrimidine
    Percent Composition: C 42....
    Literature References: Synthesis starting with ethyl ethoxyethylenecyanoacetate: Ulbricht, Price, J. Org. Chem. 21, 567 (1956).

  • Sodium Metaperiodate CAS Registry Number: 7790-28-5 高碘酸钠


    CAS Name: Sodium periodate
    Percent Composition: I 59.33%, Na 10.75%, O 29.92%
    Literature References: Synthesis starting with sodium iodide: Inorg. Synth. 2, 212 (1946) and 1, 170 (1939).

  • Phenylpropylmethylamine CAS Registry Number: 93-88-9 苯丙甲胺


    CAS Name: N,b-Dimethylbenzeneethanamine
    Additional Names: dl-N,b-dimethylphenethylamine; dl-N-methyl-2-phenylpropylamine; 1-methylamino-2-phenylpropane; phenpromethamine; 1-methylamino-2-methyl...
    Literature References: Synthesis starting with the condensation of chlorobenzene with allyl chloride, followed by ammonolysis: Patrick et al., J. Am. Chem. Soc. 68, 1009 (1946).

  • Neostigmine CAS Registry Number: 59-99-4 新斯的明


    CAS Name: 3-[[(Dimethylamino)carbonyl]oxy]-N,N,N-trimethylbenzenaminium
    Additional Names: (3-dimethylcarbamoxyphenyl) trimethylammonium; synstigmin; proserine
    Literature References: Synthesis: Aeschlimann, US 1905990 (1933 to Hoffmann-La Roche); Yanagisawa, JP 51 3071 (1951), C.A. 47, 4908g (1953). Pharmacology and pharmacokinetics: T. N. Calvey et al., Br. J. Clin. Pharmacol. 7, 149 (1979). Synergism of neostigmine toxicity by lithium: W. M. Davis, N. S. Hatoum, Toxicology 17, 1 (1980). Toxicity: L. O. Randall, G. Lehmann, J. Pharmacol. Exp. Ther. 99, 16 (1950). Comprehensive description: A. A. Al-Badr, M. Tariq, Anal. Profiles Drug Subs. 16, 403-444 (1987). Clinical evaluation in treatment of acute colonic pseudo-obstruction: R. J. Ponec et al., N. Engl. J. Med. 341, 137 (1999).

  • Coumaran CAS Registry Number: 496-16-2 2,3-二氢苯并呋喃


    CAS Name: 2,3-Dihydrobenzofuran
    Additional Names: cumaran; dihydrocoumarone
    Percent Composition: C 79.97%, H 6.71%, O 13.32%
    Literature References: Synthesis: Bennett, Mahmoud Hafez, J. Chem. Soc. 1941, 287; cf. Hurd, Hoffmann, J. Org. Chem. 5, 212 (1940); Rindfusz, J. Am. Chem. Soc. 41, 669 (1919); J. M. Bakke, H. M. Roholdt, Acta Chem. Scand. B34, 73 (1980).

  • Nealbarbital CAS Registry Number: 561-83-1 尼阿比妥


    CAS Name: 5-(2,2-Dimethylpropyl)-5-(2-propenyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
    Additional Names: 5-allyl-5-neopentylbarbituric acid; nealbarbitone; neallymal
    Trademarks: Nevental (Pharmaci...
    Literature References: Synthesis: Brandstrom, Acta Chem. Scand. 13, 613, 615, 619 (1959); GB 797017 and US 2899435 (1958, 1959, both to Pharmacia). Metabolism: J. N. T. Gilbert et al., J. Pharm. Pharmacol. 26, 119 (1974); J. N. T. Gilbert, J. W. Powell, Eur. J. Drug Metab. Pharmacokinet. 3, 195 (1978).

  • Thiamphenicol CAS Registry Number: 15318-45-3 甲砜霉素


    CAS Name: 2,2-Dichloro-N-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)-2-[4-(methylsulfonyl)phenyl]ethyl]acetamide
    Additional Names: D-d-threo-2-dichloroacetamido-1-(4-methylsulfonyl)phenyl-1,3-propaned...
    Literature References: Synthesis: Cutler et al., J. Am. Chem. Soc. 74, 5475 (1952); Suter et al., ibid. 75, 4330 (1953); Suter, US 2759927; US 2759970; US 2759971; US 2759972; US 2759976 (all 1956 to Sterling Drugs); GB 770277 (1957 to Parke, Davis).

  • Dienestrol CAS Registry Number: 84-17-3 2,3-二苯酚丁二烯


    CAS Name: 4,4'-(1,2-Diethylidene-1,2-ethanediyl)bisphenol
    Additional Names: 4,4'-(diethylideneethylene)diphenol; 3,4-bis(p-hydroxyphenyl)-2,4-hexadiene; 4,4'-dihydroxy-g,d-diphenyl-b,d-hexadien...
    Literature References: Synthesis: Dodds et al., Proc. Roy. Soc. 127B, 162 (1939); Hobday, Short, J. Chem. Soc. 1943, 609; Short, Hobday, US 2464203 (1949 to Boots); Adler, US 2465505 (1949 to Hoffmann-La Roche). Configuration: Koch, Nature 161, 309 (1948); Lane, Spialter, J. Am. Chem. Soc. 73, 4408 (1951).

  • Fenipentol CAS Registry Number: 583-03-9 1-苯基-1-戊醇


    CAS Name: a-Butylbenzenemethanol
    Additional Names: a-butylbenzyl alcohol; phenylbutylcarbinol; 1-phenyl-1-hydroxypentane; phenylpentanol; PC 1; Ph BC
    Trademarks: Pancoral (Eisai)
    Percent ...
    Literature References: Synthesis: Fourneau, Puyal, An. Soc. Esp. Fis. Quim. 18, 323 (1920); Adams, Vander Werf, J. Am. Chem. Soc. 72, 4368 (1950); Protiva et al., Chem. Listy 46, 37 (1952). Prepn of the drug: Scheffler, Engelhorn, GB 915815; eidem, US 3084100 (both 1963 to Thomae). Pharmacology: Engelhorn, Arzneim.-Forsch. 10, 255 (1960); Beck, Bierwisch, ibid. 20, 693 (1970). Metabolism: Koss et al., ibid. 14, 195 (1964).

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