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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

  • Nipradilol CAS Registry Number: 81486-22-8 尼普地洛


    CAS Name: 3,4-Dihydro-8-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]-2H-1-benzopyran-3-ol 3-nitrate
    Additional Names: 3,4-dihydro-8-(2-hydroxy-3-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran;...
    Literature References: b-Adrenergic blocker with vasodilating activity. Prepn: M. Shiratsuchi et al., EP 42299; eidem, US 4394382 (1981, 1983 both to Kowa). Synthesis: M. Shiratsuchi et al., Chem. Pharm. Bull. 35, 632 (1987). Resolution of isomers: M. Shiratsuchi et al., EP 154511; eidem, US 4727085 (1985, 1988 both to Kowa). Synthesis and activity of isomers: M. Shiratsuchi et al., Chem. Pharm. Bull. 35, 3691 (1987). Pharmacology: Y. Uchida et al., Arch. Int. Pharmacodyn. 262, 132 (1983). Hemodynamic effects in dogs: H. Hisa et al., ibid. 271, 169 (1984). Effects on cardiac function in dogs: M. Sakanashi et al., ibid. 274, 47 (1985); M. Fujii et al., Jpn. Heart J. 27, 233 (1986). Pharmacokinetics and metabolism in rats: S. Kabuto et al., Arzneim.-Forsch. 35, 1674 (1985); H. Kimata et al., ibid. 1680. Metabolic fate in dog and man: M. Yoshimura et al., Chem. Pharm. Bull. 33, 3456 (1985). Clinical evaluation in angina: H. Kishida et al., Jpn. Heart J. 29, 309 (1988).

  • Pronethalol CAS Registry Number: 54-80-8 (+/-)-前萘洛尔


    CAS Name: a-[[(1-Methylethyl)amino]methyl]-2-naphthalenemethanol
    Additional Names: a-[(isopropylamino)methyl]-2-naphthalenemethanol; [2-hydroxy-2-(2-naphthyl)ethyl]isopropylamine; 2-isopropylam...
    Literature References: b-Adrenergic blocker. Prepd by reduction of 2-naphthacyl bromide with NaBH4 followed by reaction with isopropylamine: Stephenson, GB 909357 (1962 to ICI). Pharmacology: Black et al., Br. J. Pharmacol. Chemother. 25, 577 (1965). Carcinogenicity in mice: R. Howe, Nature 207, 594 (1965). Metabolism: W. G. Stillwell, M. G. Horning, Res. Commun. Chem. Pathol. Pharmacol. 9, 601 (1974).

  • Propranolol CAS Registry Number: 525-66-6 心得安(普萘洛尔)


    CAS Name: 1-[(1-Methylethyl)amino]-3-(1-naphthalenyloxy)-2-propanol
    Additional Names: 1-(isopropylamino)-3-(1-naphthyloxy)-2-propanol
    Trademarks: Avlocardyl (AstraZeneca); Euprovasin (Magis)...
    Literature References: b-Adrenergic blocker. Prepn: BE 640312 and BE 640313; Crowther, Smith, US 3337628 and US 3520919 (1964, 1964, 1967, 1970 all to I.C.I.). Description of optical isomers: Howe, Shanks, Nature 210, 1336 (1966). Biological studies: Barrett, Cullum, Br. J. Pharmacol. 34, 43 (1968). Metabolism: Bond, Nature 213, 721 (1967). Multi-center clinical trial in myocardial infarction: V. Hansteen et al., Br. Med. J. 284, 155 (1982). Use as migraine prophylactic: S. Diamond, E. Millstein, J. Clin. Pharmacol. 28, 193 (1988); S. Diamond et al., Headache 27, 70 (1987). Toxicity data: M. Martin, P. Linee, Eur. J. Med. Chem. 9, 563 (1974). Review of pharmacokinetics: P. A. Routledge, D. G. Shand, Appl. Pharmacokinet. 1980, 464-485; of pharmacology: J. D. Fitzgerald in Pharmacology of Antihypertensive Drugs, A. Scriabine, Ed. (Raven Press, New York, 1980) pp 195-208. Series of articles on use in hypertension: Drugs 37, Suppl. 2, 42-76 (1989).

  • Oxprenolol CAS Registry Number: 6452-71-7 氧烯洛尔


    CAS Name: 1-[(1-Methylethyl)amino]-3-[2-(2-propenyloxy)phenoxy]-2-propanol
    Additional Names: 1-[o-(allyloxy)phenoxy]-3-(isopropylamino)-2-propanol; 1-(isopropylamino)-2-hydroxy-3-[o-(allyloxy)p...
    Literature References: b-Adrenergic blocker. Prepn: BE 669402 (1966 to Ciba), C.A. 65, 5402d (1966), corresp to GB 1077603. Metabolic studies: Garteiz, J. Pharmacol. Exp. Ther. 179, 354 (1971). Crystal structure of hydrochloride: J. M. Leger et al., Acta Crystallogr. 33B, 2156 (1977). Long-term prevention study in coronary heart disease: S. H. Taylor et al., N. Engl. J. Med. 307, 1293 (1982).

  • Toliprolol CAS Registry Number: 2933-94-0 托利洛尔


    CAS Name: 1-[(1-Methylethyl)amino]-3-(3-methylphenoxy)-2-propanol
    Additional Names: 1-(isopropylamino)-3-(m-tolyloxy)-2-propanol; 1-(3-methylphenoxy)-3-(isopropylamino)-2-propanol; 1-(3-methylp...
    Literature References: b-Adrenergic blocker. Prepn: NL 6409883; H. Koppe et al., US 3459782 (1965, 1969 both to Boehringer, Ing.); NL 6410522; R. Howe, US 3432545 (1965, 1969 both to I.C.I.). The (-)-isomer is the more potent adrenergic b-receptor antagonist. Resolution of isomers: Howe, Rao, J. Med. Chem. 11, 1118 (1968). Structure-activity studies: Crowther et al., ibid. 12, 638 (1969); Somani, Laddu, Eur. J. Pharmacol. 14, 209 (1971). Metabolism: Stock, Westermann, Biochem. Pharmacol. 14, 227 (1965). Review of pharmacology and clinical data: Marmo et al., Clin. Ter. 62, 11-51, 117-163 (1972).

  • Timolol CAS Registry Number: 26839-75-8 噻吗洛尔


    CAS Name: (2S)-1-[(1,1-Dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol
    Additional Names: S-(-)-3-(3-tert-butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadia...
    Literature References: b-Adrenergic blocker. Prepn: B. K. Wasson, DE 1925956; idem, US 3655663 (1969, 1972 both to Frosst). Manufacturing process: L. M. Weinstock et al., DE 1925955; eidem, US 3657237 (1970, 1972 both to Frosst). Synthesis and activity data: Wasson et al., J. Med. Chem. 15, 651 (1972). Pharmacology: Franciosa et al., Clin. Pharmacol. Ther. 13, 138 (1972); Ulrych et al., ibid. 232. Review of efficacy in glaucoma: R. C. Heel et al., Drugs 17, 38-55 (1979). Clinical evaluation in hypertension: B. A. Rofman et al., Hypertension 2, 643 (1980). Multicenter study of effect in myocardial infarction: N. Engl. J. Med. 304, 801 (1981); of efficacy in limiting infarct size: M. Sederholm et al., ibid. 310, 9 (1984). Comprehensive description: D. J. Mazzo, A. E. Loper, Anal. Profiles Drug Subs. 16, 641-692 (1987).

  • Alprenolol CAS Registry Number: 13655-52-2 阿普洛尔


    CAS Name: 1-[(1-Methylethyl)amino]-3-[2-(2-propenyl)phenoxy]-2-propanol
    Additional Names: 1-(o-allylphenoxy)-3-(isopropylamino)-2-propanolPercent Composition: C 72.25%, H 9.30%, N 5.62%, O 12.8...
    Literature References: b-Adrenergic blocker. Prepn: Brandstrom et al., Acta Pharm. Suec. 3, 303 (1966); NL 6605692 (1966 to AB Hassle), C.A. 66, 46214p (1967); NL 6612958 (1967 to ICI), C.A. 67, 99851w (1967). Pharmacology: Marmo, Clin. Ter. 56, 121-176 (1971). Series of articles on clinical effect in myocardial infarction: Acta Med. Scand. 1984, Suppl. 680, 1-64.

  • Moprolol CAS Registry Number: 5741-22-0 莫普洛尔


    CAS Name: 1-(2-Methoxyphenoxy)-3-[(1-methylethyl)amino]-2-propanol
    Additional Names: 1-(isopropylamino)-3-(o-methoxyphenoxy)-2-propanol
    Percent Composition: C 65.25%, H 8.84%, N 5.85%, O 20....
    Literature References: b-Adrenergic blocker. Prepn: C. D. Lunsford et al., J. Am. Chem. Soc. 82, 1166 (1960); NL 301580 corresp to A. F. Crowther, L. H. Smith, US 3501769 (1965, 1970 both to ICI); A. F. Crowther et al., J. Med. Chem. 12, 638 (1969). Pharmacology: G. Croce et al., Arzneim.-Forsch. 20, 1074 (1970). Anti-anginal and hemodynamic effects: M. Radice et al., ibid. 28, 2160 (1978). Resolution of enantiomers: G. Ferrari, V. Vecchietti, EP 15418; eidem, US 4683245 (1980, 1987 both to Simes). Synthesis of (-)-form: K. Kan et al., Agric. Biol. Chem. 49, 207 (1985). Bioavailability of (-)-form in dog: A. Marzo, J. P. Desager, Curr. Ther. Res. 30, 442 (1981). Pharmacokinetics of racemate and (-)-form: C. Harvengt, J. P. Desager, Int. J. Clin. Pharmacol. Ther. Toxicol. 20, 57 (1982). Clinical comparison of antihypertensive activity of enantiomers: P. Ghirardi, F. Grosso, J. Cardiovasc. Pharmacol. 2, 471 (1980). Clinical studies of (-)-form in hypertension: G. Vrebos et al., Curr. Ther. Res. 29, 654 (1981); H. Hoeffkes, ibid. 30, 88 (1981).

  • Nadolol CAS Registry Number: 42200-33-9 苯甲丁氮酮


    CAS Name: 5-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-1,2,3,4-tetrahydro-2,3-naphthalenediol
    Additional Names: 1-(tert-butylamino)-3-[(5,6,7,8-tetrahydro-cis-6,7-dihydroxy-1-naphthyl)oxy]...
    Literature References: b-Adrenergic blocker. Prepn: F. P. Hauck et al., DE 2258995; eidem, US 3935267 (1973, 1976, both to Squibb). Resolution of isomers: F. P. Hauck, J. E. Sundeen, DE 2421549 (1974 to Squibb), C.A. 82, 57481e (1975). Metabolism: J. Dreyfuss et al., J. Clin. Pharmacol. 17, 300 (1977). Toxicology: P. L. Sibley et al., Toxicol. Appl. Pharmacol. 44, 379 (1978). Review of pharmacology: R. C. Heel et al., Drugs 1, 1-23 (1980); M. J. Antonaccio, D. B. Evans, in Pharmacology of Antihypertensive Drugs, A. Scriabine, Ed. (Raven Press, New York, 1980) pp 295-301. Comprehensive description: L. Slusarek, K. Florey, Anal. Profiles Drug Subs. 9, 455-485 (1980). Book: International Experience with Nadolol, a Long-Acting b-Blocking Agent, F. Gross, Ed. (Grune Stratton, New York, 1981) 229 pp.

  • Butidrine Hydrochloride CAS Registry Number: 1506-12-3 布替君盐酸盐


    CAS Name: 5,6,7,8-Tetrahydro-a-[[(1-methylpropyl)amino]methyl]-2-naphthalenemethanol hydrochloride
    Additional Names: a-[(sec-butylamino)methyl]-5,6,7,8-tetrahydro-2-naphthalenemethanol hydrochl...
    Literature References: b-Adrenergic blocker. Prepn: Ferrari et al., Boll. Chim. Farm. 103, 32 (1964), C.A. 61, 5580d (1964); FR 1390056 (1965 to Holding Ceresia), C.A. 62, 16162d (1965). Pharmacology: R. Ferrini, Arzneim.-Forsch. 18, 48 (1968). Brief review of butidrine and other b-blockers: A. M. Karow et al., Prog. Drug Res. 15, 103-122 (1971).

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