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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

  • Nadoxolol CAS Registry Number: 54063-51-3 N,3-二羟基-4-(萘-1-基氧基)丁酰胺


    CAS Name: N,3-Dihydroxy-4-(1-naphthalenyloxy)butanimidamide
    Additional Names: 3-hydroxy-4-(1-naphthyloxy)butyramidoxime; 4-(a-naphthyloxy)-3-hydroxybutyramidoxime
    Percent Composition: C 64.6...
    Literature References: b-Adrenergic blocker. Prepn: Lafon, DE 2132113 corresp to US 3819702 (1972, 1974 to Orsymonde). Pharmacology: Duteil et al., Therapie 28, 703 (1973). Clinical studies: Tricot et al., ibid. 721.

  • Bufetolol CAS Registry Number: 53684-49-4 布非洛尔


    CAS Name: 1-[(1,1-Dimethylethyl)amino]-3-[2-[(tetrahydro-2-furanyl)methoxy]phenoxy]-2-propanol
    Additional Names: 1-(tert-butylamino)-3-[o-[(tetrahydrofurfuryl)oxy]phenoxy]-2-propanol
    Percent...
    Literature References: b-Adrenergic blocker. Prepn: M. Nakanishi et al., DE 2024001; eidem, US 3723476 (1970, 1973, both to Yoshitomi); eidem, J. Med. Chem. 15, 45 (1972). Pharmacology: M. Nakanishi et al., Yakugaku Zasshi 91, 1037 (1971); ibid. 92, 375 (1972); Imamura et al., ibid. 1039. Metabolism: M. Nakanishi et al., ibid. 299; Oyo Yakuri 6, 479 (1972), C.A. 78, 66785b (1973). Toxicology: eidem, ibid. 485, 1267, C.A. 78, 66945d; 79, 337w (1973).

  • Sulfinalol CAS Registry Number: 66264-77-5 硫氧洛尔


    CAS Name: 4-Hydroxy-a-[[[3-(4-methoxyphenyl)-1-methylpropyl]amino]methyl]-3-(methylsulfinyl)benzenemethanol
    Additional Names: 4-hydroxy-a-[[[3-(p-methoxyphenyl)-1-methylpropyl]amino]methyl]-3-(...
    Literature References: b-Adrenergic blocker. Prepn: R. E. Philion, DE 2728641 (1978 to Sterling), C.A. 90, 137468 (1979). Pharmacological activity profile: P. H. Hernández, Fed. Proc. 38, 738 (1979). Chromatographic determn in human plasma and urine: G. B. Park et al., Anal. Chem. 53, 604 (1981). Metabolism, disposition in animals: D. P. Benziger et al., Drug Metab. Dispos. 9, 493 (1981).

  • Nifenalol CAS Registry Number: 7413-36-7 硝苯洛尔


    CAS Name: a-[[(1-Methylethyl)amino]methyl]-4-nitrobenzenemethanol
    Additional Names: a-[(isopropylamino)methyl]-p-nitrobenzyl alcohol; 1-(4-nitrophenyl)-2-(isopropylamino)ethanol; isophenethanol...
    Literature References: b-Adrenergic blocker. Prepn: Teotino et al., Farmaco Ed. Sci. 17, 252 (1962); eidem, GB 950682 (1964 to Selvi), C.A. 60, 13184h (1964). Pharmacology: Somani, Lum, J. Pharmacol. Exp. Ther. 147, 194 (1965); Almirante et al., Farmaco Ed. Sci. 21, 637 (1966). Prepn of the optical isomers: Almirante, Murmann, J. Med. Chem. 9, 650 (1966); eidem, BE 673273 (1966 to Selvi), C.A. 66, 65278d (1967).

  • Sotalol CAS Registry Number: 3930-20-9 索他洛尔


    CAS Name: N-[4-[1-Hydroxy-2-[(1-methylethyl)amino]ethyl]phenyl]methanesulfonamide
    Additional Names: 4'-[1-hydroxy-2-(isopropylamino)ethyl]methanesulfonanilide
    Percent Composition: C 52.92%, ...
    Literature References: b-Adrenergic blocker. Prepn: Uloth et al., J. Med. Chem. 9, 88 (1966). Pharmacology and toxicology: Larsen, Lish, Nature 203, 1283 (1964); Lish et al., J. Pharmacol. Exp. Ther. 149, 161 (1965); Stanton et al., ibid. 175; Kvam et al., ibid. 183. Activity of the d- and l-forms: Somani, Watson, ibid. 164, 317 (1968); Somani, Bachand, Eur. J. Pharmacol. 7, 239 (1969). HPLC determn in body fluids: W. P. Gluth et al., Arzneim.-Forsch. 38, 408 (1988). Review of pharmacology and therapeutic use: B. N. Singh et al., Drugs 34, 311-349 (1987); S. H. Hohnloser, R. L. Woosley, N. Engl. J. Med. 331, 31-38 (1994). Comprehensive description: R. T. Foster, R. A. Carr, Anal. Profiles Drug Subs. Excip. 21, 501-533 (1992).

  • Bucumolol CAS Registry Number: 58409-59-9 香豆心安


    CAS Name: 8-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-5-methyl-2H-1-benzopyran-2-one
    Additional Names: (±)-8-[3-(t-butylamino)-2-hydroxypropoxy]-5-methylcoumarin; dl-8-(2-hydroxy-3-t...
    Literature References: b-Adrenergic blocker. Prepn: Y. Sato et al., DE 2021958; eidem, US 3663570 (1970, 1972 both to Sankyo); eidem, Chem. Pharm. Bull. 20, 905 (1972). Pharmacology: T. Oshima et al., Jpn. J. Pharmacol. 23, 497 (1973). Metabolic studies: R. Hayashi et al., Chem. Pharm. Bull. 23, 1173 (1975). Antiarrhythmic activity in dogs: K. Nakayama et al., Jpn. J. Pharmacol. 29, 935 (1979). Early clinical study: H. Kishida et al., Rinsho Yakuri 11, 99 (1980), C.A. 93, 107380w (1980).

  • Mepindolol CAS Registry Number: 23694-81-7 甲吲哚心安


    CAS Name: 1-[(1-Methylethyl)amino]-3-[(2-methyl-1H-indol-4-yl)oxy]-2-propanol
    Additional Names: 1-(isopropylamino)-3-[(2-methylindol-4-yl)oxy]-2-propanol
    Percent Composition: C 68.67%, H 8.4...
    Literature References: b-Adrenergic blocker; the 2-methyl analog of pindolol, q.v. Prepn: F. Troxler, CH 469002 and CH 472404 (both 1969 to Sandoz); F. Seeman et al., Helv. Chim. Acta 54, 2411 (1971). Pharmacokinetics: R. Gugler et al., Arzneim.-Forsch. 25, 1067 (1975). Pharmacodynamics: J. Bonelli et al., Eur. J. Clin. Pharmacol. 15, 1 (1979). Clinical studies: H. M. Beumer et al., Int. J. Clin. Pharmacol. Biopharm. 16, 249 (1978); M. Sukerman et al., Curr. Ther. Res. 25, 384 (1979).

  • Storax CAS Registry Number: 8023-62-9 苏合香酯


    Additional Names: Styrax; sweet oriental gum
    Literature References: Balsam obtained from the trunk of Liquidambar orientalis Mill., known as Levant Storax, or of L. styraciflua L., known as American Storax (family Hamamelidaceae). Habit. Levant storax is native to Asia Minor. American storax is produced chiefly in Honduras; found along the Atlantic coast from Connecticut to Central America. Constit. 33-50% a- and b-storesin and its cinnamic ester; 5-10% styracin; 10% phenylpropyl cinnamate; small amounts of ethyl cinnamate; benzyl cinnamate; 5-15% free cinnamic acid; styrene; 0.4% levorotatory oil; C10H16O, and traces of vanillin.

  • Tricromyl CAS Registry Number: 85-90-5 3-甲基-4h-色烯-4-酮


    CAS Name: 3-Methyl-4H-1-benzopyran-4-one
    Additional Names: 3-methylchromone; 3-methyl-g-benzopyrone
    Trademarks: Cromonalgina (Ceccarelli)
    Percent Composition: C 74.99%, H 5.03%, O 19.98%
    Literature References: Based on an ancient Egyptian drug now termed bezr el khelda. Prepn from o-hydroxypropiophenone: Clerc-Bory et al., Bull. Soc. Chim. Fr. 1955, 1083; Mentzer, Meunier, FR 980785 (1951 to Lab. Franc. Chimiother.); Mentzer, US 2769015 (1956 one-half to Laroche-Navarron).

  • Canavanine CAS Registry Number: 543-38-4 L-刀豆氨酸


    CAS Name: O-[(Aminoiminomethyl)amino]homoserine
    Additional Names: 2-amino-4-(guanidinooxy)butyric acid
    Percent Composition: C 34.09%, H 6.87%, N 31.80%, O 27.25%
    Literature References: Basic amino acid isolated as L-canavanine from jack beans, Canavalia ensiformis (L.) DC., Leguminosae: Kitagawa, Tomiyama, J. Biochem. (Tokyo) 11, 265 (1929). Constitutes about 1.5% of the dry weight of alfalfa seeds and sprouts: E. A. Bell Biochem. J. 75, 618 (1960). Distribution in the plant kingdom: Turner, Harborne, Phytochemistry 6, 863 (1967). Structure: Gulland, Morris, J. Chem. Soc. 1935, 763; Kitagawa, Takani, J. Biochem. (Tokyo) 23, 181 (1936). Configuration: Cadden, Proc. Soc. Exp. Biol. Med. 45, 224 (1940). Synthesis of racemate: Nyberg, Christensen, J. Am. Chem. Soc. 79, 1222 (1957); Frankel et al., J. Chem. Soc. 1963, 3127. Alternate synthesis: Yamada et al., Agric. Biol. Chem. 37, 2201 (1973). Bears resemblance to arginine, q.v. and is often used as substrate to some enzymes normally acting on arginine. Accordingly it is a potent growth inhibitor of many organisms: Pilcher et al., Proc. Soc. Exp. Biol. Med. 88, 79 (1955). Toxic to mammals: B. Tschiersch, Pharmazie 17, 621 (1962). L-Canavanine induces certain hematologic and serologic abnormalities characteristic of systemic lupus erythematosus in monkeys: M. R. Malinow et al., Science 216, 415 (1982).

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