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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

  • Thonzylamine Hydrochloride CAS Registry Number: 63-56-9 盐酸嘧啶二胺


    CAS Name: N-[(4-Methoxyphenyl)methyl]-N',N'-dimethyl-N-2-pyrimidinyl-1,2-ethanediamine monohydrochloride
    Additional Names: 2-[(2-dimethylaminoethyl)(p-methoxybenzyl)amino]pyrimidine hydrochlori...
    Literature References: Histamine H1-receptor antagonist. Prepd by treating the sodium salt of 2-(p-methoxybenzyl)aminopyrimidine with N,N-dimethyl-2-chloroethylamine: Friedman, Tolstoouhov, US 2465865 (1949). Toxicity study: Reinhard, Seudi, Proc. Soc. Exp. Biol. Med. 66, 512 (1947). Spectroscopic determn in nasal drops: S. M. Sabry et al., J. Pharm. Biomed. Anal. 22, 257 (2000).

  • Bepotastine CAS Registry Number: 190786-43-7 贝他斯汀


    CAS Name: 4-[(S)-(4-Chlorophenyl)-2-pyridinylmethoxy]-1-piperidinebutanoic acid
    Additional Names: betotastine
    Percent Composition: C 64.86%, H 6.48%, Cl 9.12%, N 7.20%, O 12.34%
    Literature References: Histamine H1-receptor antagonist. Prepn (stereochem. unspec.): A. Koda et al., EP 335586; eidem, US 4929618 (1989, 1990 both to Ube). Prepn of optically active salts: J. Kita et al., EP 949260 (1999 to Ube; Tanabe Seiyaku). Pharmacology: M. Kato et al., Arzneim.-Forsch. 47, 1116 (1997). Suppression of IL-5 production: O. Kaminuma et al., Biol. Pharm. Bull. 21, 411 (1998). Antiallergic activity in animal models: M. Ueno et al., Pharmacology 57, 206 (1998).

  • Triprolidine CAS Registry Number: 486-12-4 曲普立定


    CAS Name: 2-[(1E)-1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]pyridine
    Additional Names: trans-2-[3-(1-pyrrolidinyl)-1-p-tolylpropenyl]pyridine; trans-1-(2-pyridyl)-3-pyrrolidino-1-p-tolyl...
    Literature References: Histamine H1-receptor antagonist. Prepn: Adamson, US 2712020; US 2712023 (both 1955 to Burroughs Wellcome); Adamson et al., J. Chem. Soc. 1958, 312. Structure-activity studies: Ison, Casy, J. Pharm. Pharmacol. 23, 848 (1971). Crystal and molecular structure: James, Williams, Can. J. Chem. 52, 1880 (1974). Pharmacokinetics and antihistaminic effects in humans: K. J. Simons et al., J. Allergy Clin. Immunol. 77, 326 (1986). Comprehensive description: S. A. Benezra, C.-H. Yang, Anal. Profiles Drug Subs. 8, 509-528 (1979).

  • Emedastine CAS Registry Number: 87233-61-2 依美司丁


    CAS Name: 1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole
    Additional Names: 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-homopiperazinyl)benzimidazole
    Percent Composition...
    Literature References: Histamine H1-receptor antagonist. Prepn: R. Iemura et al., EP 79545; eidem, US 4430343 (1983, 1984 both to Kanebo); eidem, J. Med. Chem. 29, 1178 (1986). GC determn in plasma: T. Hamada et al., Chem. Pharm. Bull. 34, 1168 (1986). Series of articles on pharmacology: Arzneim.-Forsch. 34, 801-818 (1984). Toxicity data: T. Fukuda et al., ibid. 801.

  • Nizatidine CAS Registry Number: 76963-41-2 尼扎替丁


    CAS Name: N-[2-[[[2-[(Dimethylamino)methyl]-4-thiazolyl]methyl]thio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine
    Additional Names: N-[4-(6-methylamino-7-nitro-2-thia-5-aza-6-heptene-1-yl)-2-thiaz...
    Literature References: Histamine H2-receptor antagonist related to ranitidine, q.v. Prepn: R. P. Pioch, EP 49618; idem, US 4375547 (1982, 1983 both to Eli Lilly). General pharmacology in animals: K. Bemis et al., Arzneim.-Forsch. 39, 240 (1989). Pharmacokinetics and gastric acid suppression in humans: J. T. Callaghan et al., Clin. Pharmacol. Ther. 37, 162 (1985). Study of effect on hepatic drug metabolism in humans: J. W. Secor et al., Br. J. Clin. Pharmacol. 20, 710 (1985). Disposition and metabolism in humans: M. P. Knadler et al., Drug Metab. Dispos. 14, 175 (1986). Symposium on pharmacology and clinical studies: Scand. J. Gastroenterol. 22, Suppl. 136, 1-88 (1987). Comprehensive description: T. J. Wozniak, Anal. Profiles Drug Subs. 19, 397-427 (1990).

  • Ranitidine CAS Registry Number: 66357-35-5 雷尼替丁


    CAS Name: N-[2-[[[-5-[(Dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine
    Percent Composition: C 49.66%, H 7.05%, N 17.82%, O 15.27%, S 10.20%
    Literature References: Histamine H2-receptor antagonist which inhibits gastric acid secretion. Prepn: B. J. Price et al., FR 2384765; eidem, US 4128658 (both 1978 to Allen Hanburys). HPLC determn in plasma: P. F. Carey, L. E. Martin, J. Liq. Chromatogr. 1979, 1291. Pharmacological studies: J. Bradshaw et al., Br. J. Pharmacol. 66, 464 (1979); M. J. Daly et al., Gut 21, 408 (1980). Efficacy in treatment of duodenal ulcers: A. Berstad et al., Scand. J. Gastroenterol. 15, 637 (1980); R. P. Walt et al., Gut 22, 49 (1981). Review of pharmacology and therapeutic use: R. N. Brogden et al., Drugs 24, 267-303 (1982). Comprehensive description: M. Hohnjec et al., Anal. Profiles Drug Subs. 15, 533-561 (1986).

  • Roxatidine Acetate CAS Registry Number: 78628-28-1 醋酸罗沙替丁


    CAS Name: 2-(Acetyloxy)-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]acetamide
    Additional Names: aceroxatidine
    Percent Composition: C 65.49%, H 8.10%, N 8.04%, O 18.37%
    Literature References: Histamine H2-receptor antagonist. Prepn and anti-ulcerative activity: K. Shibata et al., EP 24510; eidem, US 4293557 (both 1981 to Teikoku Hormone). Pharmacology in animals: M. Tarutani et al., Arzneim.-Forsch. 35, 703 (1985). Comparison with cimetidine of effect on gastric acid secretion and ulcer formation in animals: eidem, ibid. 844. Metabolism in humans: S. Honma et al., Oyo Yakuri 30, 555 (1985); C.A. 104, 61453n (1985).

  • Famotidine CAS Registry Number: 76824-35-6 法莫替丁


    CAS Name: 3-[[[2-[(Aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]-N-(aminosulfonyl)propanimidamide
    Additional Names: [1-amino-3-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]propylid...
    Literature References: Histamine H2-receptor antagonist. Prepn, NMR and mass spectral data: H. Yasufumi et al., BE 882071; eidem, US 4283408; JP Kokai 81 55383, C.A. 95, 203930n (1980, 1981, 1981 all to Yamanouchi). Inhibition of gastric acid and pepsin secretion in rats: M. Takeda et al., Arzneim.-Forsch. 32, 734 (1982); in man: M. Miwa et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 22, 214 (1984). Effect on disposition of antipyrine in liver: Ch. Staiger et al., Arzneim.-Forsch. 34, 1041 (1984). Chromatographic determn in plasma and urine: W. C. Vincek et al., J. Chromatogr. 338, 438 (1985). Pharmacokinetics: T. Takabatke et al., Eur. J. Clin. Pharmacol. 28, 327 (1985). Clinical trial in Zollinger-Ellison syndrome: J. M. Howard et al., Gastroenterology 88, 1026 (1985). Symposia on pharmacology and clinical efficacy: Am. J. Med. 81, Suppl. 4B, 1-64 (1986); Scand. J. Gastroenterol. 22, Suppl. 134, 1-62 (1987).

  • Ebrotidine CAS Registry Number: 100981-43-9 乙溴替丁


    CAS Name: N-[[[2-[[[2-[(Aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl]amino]methylene]-4-bromobenzenesulfonamide
    Additional Names: N-p-bromobenzenesulfonyl-N'-[2-[[[2-[(aminoiminomethyl...
    Literature References: Histamine H2-receptor antagonist. Prepn: R. Foguet et al., EP 159012; eidem, US 4728655 (1985, 1988 both to Ferrer); L. Anglada et al., Eur. J. Med. Chem. 23, 97 (1988). Clinical pharmacology: S. J. Konturek et al., Scand. J. Gastroenterol. 27, 438 (1992); M. Maczka et al., J. Physiol. Pharmacol. 43, 139 (1992). Clinical evaluation in gastroesophageal reflux disease: E. Sito et al., ibid. 44, 259 (1993). HPLC determn in urine and metabolism study: E. Rozman et al., J. Pharm. Sci. 83, 252 (1994).

  • Nelfinavir CAS Registry Number: 159989-64-7 奈非那韦


    CAS Name: (3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide
    Additional Names: [3S-(3R*,4aR*,8a...
    Literature References: HIV protease inhibitor. Prepn: B. A. Dressman et al., WO 9509843; eidem, US 5484926 (1995, 1996 both to Agouron). Physical properties: M. Longer et al., J. Pharm. Sci. 84, 1090 (1995). HIV protease inhibition and antiviral activity: A. K. Patick et al., Antimicrob. Agents Chemother. 40, 292 (1996). Preclinical pharmacokinetics and tissue distribution: B. V. Shetty et al., ibid. 110. Review of pharmacology and clinical efficacy in HIV infection: A. Bardsley-Elliot, G. L. Plosker et al., Drugs 59, 581-620 (2000).

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