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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

  • Phenglutarimide CAS Registry Number: 1156-05-4 芬格鲁胺


    CAS Name: 3-[2-(Diethylamino)ethyl]-3-phenyl-2,6-piperidinedione
    Additional Names: 2-(2-diethylaminoethyl)-2-phenylglutarimide; a-phenyl-a-(diethylaminoethyl)glutarimide; 3-phenyl-3-(b-diethyla...
    Literature References: Anticholinergic. Prepn: Tagmann et al., Helv. Chim. Acta 35, 1235 (1952); 37, 185 (1954); Hoffmann, Tagmann, US 2664424 (1953 to Ciba).

  • Fentonium Bromide CAS Registry Number: 5868-06-4 芬托溴铵


    CAS Name: [3(S)-endo]-8-(2-[1,1'-Biphenyl]-4-yl-2-oxoethyl)-3-(3-hydroxy-1-oxo-2-phenylpropoxy)-8-methyl-8-azoniabicyclo[3.2.1]octane bromide
    Additional Names: 3a-hydroxy-8-(p-phenylphenacyl)-1...
    Literature References: Anticholinergic. Prepn: U. Teotino, D. Della Bella, GB 1026640; eidem, US 3356682 (1966, 1967 both to Whitefin Holding); Teotino et al., Chim. Ther. 3, 453 (1968). Human pharmacology: Azzollini et al., Curr. Ther. Res. 12, 734 (1970). Clinical studies: Alberto et al., Minerva Med. 62, 852 (1971).

  • Anisotropine Methylbromide CAS Registry Number: 80-50-2 溴甲辛托品


    CAS Name: endo-8,8-Dimethyl-3-[(1-oxo-2-propylpentyl)oxy]-8-azoniabicyclo[3.2.1]octane bromide
    Additional Names: 3a-hydroxy-8-methyl-1aH,5aH-tropanium bromide 2-propylvalerate; 8-methyltropiniu...
    Literature References: Anticholinergic. Prepn: Weiner, Gordon, US 2962499 (1960 to Endo Labs.). Metabolism: Shindo et al., Chem. Pharm. Bull. 19, 513 (1971). Clinical trial in ulcer: J. H. Bowers et al., J. Clin. Pharmacol. 18, 365 (1978).

  • Trihexyphenidyl Hydrochloride CAS Registry Number: 52-49-3 盐酸苯海索


    CAS Name: a-Cyclohexyl-a-phenyl-1-piperidinepropanol hydrochloride
    Additional Names: 3-(1-piperidyl)-1-cyclohexyl-1-phenyl-1-propanol hydrochloride; 1-phenyl-1-cyclohexyl-3-piperidyl-1-propanol...
    Literature References: Anticholinergic. Synthesis: Denton et al., J. Am. Chem. Soc. 71, 2053 (1949); Adamson, Wilkinson, US 2682543 (1954 to Burroughs Wellcome); Denton, US 2716121 (1955 to Am. Cyanamid). Resolution into isomers: Adamson, Duffin, GB 750156 (1956 to Wellcome Found.).

  • Dicyclomine CAS Registry Number: 77-19-0 [联环己烷]-1-羧酸 2-(二乙基氨基)乙基酯


    CAS Name: [1,1'-Bicyclohexyl]-1-carboxylic acid 2-(diethylamino)ethyl ester
    Additional Names: b-diethylaminoethyl 1-cyclohexylcyclohexanecarboxylate; bis(cyclohexyl)carboxylic acid diethylamino...
    Literature References: Anticholinergic; binds to muscarinic M1 receptors. Prepn: C. H. Tilford et al., J. Am. Chem. Soc. 69, 2903 (1947); M. G. Van Campen, C. H. Tilford, US 2474796 (1949 to Merrell). Receptor binding study: H. Kilbinger, A. Stein, Br. J. Pharmacol. 94, 1270 (1988). Capillary GC determn in plasma: B. J. Walker et al., J. Chromatogr. 416, 150 (1987). Clinical trial in functional abdominal pain: M. G. Grillage et al., Br. J. Clin. Pract. 44, 176 (1990).

  • Hirudin CAS Registry Number: 8001-27-2 重组水蛭素 来源于酵母


    Trademarks: Exhirud (Sanofi Winthrop); Hirudex (Cooper)
    Literature References: Anticoagulant protein extracted from the salivary glands of the medicinal leech, Hirudo medicinalis Linn. Hirudin is a single chain polypeptide containing 65 amino acids; mol wt approximately 7000 daltons. Several isoforms have been identified. A specific inhibitor of thrombin, q.v., hirudin does not require the presence of other coagulation factors. Isoln: J. B. Haycraft, Arch. Exp. Pathol. Pharmakol. 18, 209 (1884). Initial characterization: F. Markwardt, Naturwissenschaften 42, 537 (1955). Improved isoln: P. Walsmann, F. Markwardt, Thromb. Res. 40, 563 (1985). Amino acid sequence: T. E. Petersen et al. in Protides of the Biological Fluids vol. 23, H. Peeters, Ed. (Pergamon Press, London, 1976) pp 145-149. Antithrombin activity: F. Markwardt, Methods Enzymol. 19, 924 (1970). Pharmacokinetics in humans: F. Markwardt et al., Thromb. Haemostasis 52, 160 (1984). Chromogenic assay in plasma: U. Griessbach et al., Thromb. Res. 37, 347 (1985). Series of articles on development, pharmacology, and therapeutic potential of natural and recombinant hirudins: Semin. Thromb. Hemostasis 15, 261-333 (1989). Review of pharmacology and therapeutic potential: P. H. Johnson, Annu. Rev. Med. 45, 165-177 (1994); of therapeutic use in myocardial infarction: U. Zeymer, K.-L. Neuhaus, Drug Saf. 12, 234-239 (1995).

  • Sodium Citrate CAS Registry Number: 68-04-2 柠檬酸钠


    CAS Name: 2-Hydroxy-1,2,3-propanetricarboxylic acid trisodium salt
    Additional Names: trisodium citrate
    Trademarks: Citrosodine (GSK); Cystemme (Abbott); Urisal (Sanofi-Synthelabo)
    Percent...
    Literature References: Anticoagulant use in blood transfusion: R. Weil, J. Am. Med. Assoc. 64, 425 (1915); cf. ibid. 250, 1901 (1983). Toxicity study: C. M. Gruber, Jr., W. A. Halbeisen, J. Pharmacol. Exp. Ther. 94, 65 (1948). Clinical evaluation of antacid efficacy: C. P. Gibbs et al., Anesthesiology 57, 44 (1982); of effects on athletic performance: V. Oöpik et al., Br. J. Sports Med. 37, 485 (2003).

  • Meobentine CAS Registry Number: 46464-11-3 甲氧苯汀


    CAS Name: N-[(4-Methoxyphenyl)methyl]-N',N''-dimethylguanidine
    Additional Names: 1-(p-methoxybenzyl)-2,3-dimethylguanidine
    Percent Composition: C 63.74%, H 8.27%, N 20.27%, O 7.72%
    Literature References: Antidysrhythmic, antifibrillatory deriv of guanidine, q.v. Prepn of the sulfate: R. A. Maxwell, E. Walton, DE 2030693 corresp to US 3949089 (1971, 1976 both to Burroughs Wellcome). Antidysrhythmic effects and tissue concentration: K. B. Touw et al., Pharmacologist 19, 268 (1977); K. B. Touw, Diss. Abstr. B 39, 5340 (1979). Pharmacokinetics by radioimmunoassay: J. W. A. Findlay et al., Pharmacologist 21, 337 (1979). Pharmacological study: W. B. Wastila et al., J. Pharm. Pharmacol. 33, 594 (1981).

  • Suclofenide CAS Registry Number: 30279-49-3 琥氯非尼


    CAS Name: 3-Chloro-4-(2,5-dioxo-3-phenyl-1-pyrrolidinyl)benzenesulfonamide
    Additional Names: 3-chloro-4-(phenylsuccinimido)benzenesulfonamide; 1-(a-phenylsuccinimido)-2-chloro-4-sulfamoylbenzen...
    Literature References: Anti-epileptic agent. Prepn: R. W. Pfirrmann, BE 752109; idem, US 3789056 (1970, 1974 both to Geistlich). Pharmacology: Arzneim.-Forsch. 27, 1942 (1977). HPLC determn in biological materials: F. Mikes et al., ibid. 29, 1583 (1979).

  • Rufinamide CAS Registry Number: 106308-44-5 卢非酰胺


    CAS Name: 1-[(2,6-Difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide
    Additional Names: 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamideTrademarks: Inovelon (Eisai)
    Percent Composit...
    Literature References: Antiepileptic triazole derivative which decreases firing by neurons at sodium channels. Prepn: R. Meier, EP 199262; eidem, US 4789680 (1986, 1988 both to Ciba-Geigy). HPLC determn in human plasma: L. A. Brunner, M. L. Powell, Biomed. Chromatogr. 6, 278 (1992). Clinical pharmacokinetics: W. K. Cheung et al., Pharm. Res. 12, 1878 (1995); and tolerability: J.-M. Cardot et al., Biopharm. Drug Dispos. 19, 259 (1998). Clinical study in epilepsy: S. Palhagen et al., Epilepsy Res. 43, 115 (2001). Review of clinical experience: K. K. Jain et al., Exp. Opin. Invest. Drugs 9, 829-840 (2000).

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