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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

  • Phenoxyacetyl Cellulose CAS Registry Number: 68332-77-4 苯氧乙酰纤维素


    CAS Name: Cellulose phenoxyacetate
    Trademarks: Enzorb-A (Regis)
    Literature References: Support used to immobilize proteins, enzymes and microsomes by hydrophobic adsorption. The attractive forces between the hydrophobic phenoxyacetate groups of the support and the hydrophobic surface areas of protein molecules arise from the common repulsion of the aqueous medium. Prepn and properties: L. G. Butler, Arch. Biochem. Biophys. 171, 645 (1975). Applications: J. Dixon et al., Biotechnol. Bioeng. 21, 2113 (1979).

  • Delmopinol CAS Registry Number: 79874-76-3 地莫匹醇


    CAS Name: 3-(4-Propylheptyl)-4-morpholineethanol
    Percent Composition: C 70.80%, H 12.25%, N 5.16%, O 11.79%
    Literature References: Surface-active agent that reduces dental plaque formation. Prepn: BE 888052; S. E. H. Hernestam et al., US 4636382 (1981, 1987 both to Ferrosan). Stereoselective HPLC determn in plasma: G. Egginger et al., J. Chromatogr. A 666, 275 (1994). In vitro effect on bacterial cell walls: J. Rundegren et al., Oral Microbiol. Immunol. 10, 102 (1995). Home usage trials of mouthwash: A. J. Elworthy et al., J. Clin. Periodontol. 22, 527 (1995); N. Claydon et al., ibid. 23, 220 (1996).

  • Hexanitrohexaazaisowurtzitane CAS Registry Number: 135285-90-4 六硝基六氮杂异伍兹烷


    CAS Name: Octahydro-1,3,4,7,8,10-hexanitro-5,2,6-(iminomethenimino)-1H-imidazo[4,5-b]pyrazine
    Additional Names: CL-20; HNIW; 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.05,9.0...
    Literature References: Symmetric polyazacyclic nitramine explosive. Polymorphs a, b, g, e, z have been identified and confirmed by x-ray diffraction or IR techniques. A sixth polymorph d has been identified, but not confirmed. First synthesized by A. T. Nielsen in 1987; modified by R. Wardle and J. C. Hinshaw. Gas phase dissociation: R. J. Doyle, Jr., Org. Mass Spectrom. 26, 723 (1991). EPR spectra: M. D. Pace, J. Phys. Chem. 95, 5858 (1991). Identification of d polymorph by high-pressure phase transition and verification of z by ir: T. P. Russell et al., ibid. 96, 5509 (1992). Pressure-temperature phase diagrams: eidem, ibid. 97, 1993 (1993). Thermal decomposition: J. C. Oxley et al., ibid. 98, 7004 (1994). High-pressure/thermal shock matrix isolation deflagration and detonation study: J. K. Rice, T. P. Russell, Chem. Phys. Lett. 234, 195 (1995). Review: S. Borman, Chem. Eng. News 72, 18-22 (Jan. 17, 1994).

  • Amezinium Methyl Sulfate CAS Registry Number: 30578-37-1 甲磺美嗪


    CAS Name: 4-Amino-6-methoxy-1-phenylpyridazinium methyl sulfateTrademarks: Regulton (Knoll); Risumic (Dainippon); Supratonin (Grñenthal)
    Percent Composition: C 46.00%, H 4.83%, N 13.41%, O 25.5...
    Literature References: Sympathomimetic agent with vascular and cardiac activity. Prepn: F. Richenender, R. Kropp, DE 1912941; eidem, US 3631038 (1970, 1971 both to BASF). Series of articles on synthesis, pharmacology, mechanism of action, metabolism, pharmacokinetics, bioavailability, clinical trials: Arzneim.-Forsch. 31, 1527-1671 (1981). Acute toxicity data: H. J. Teschendorf, ibid. 1580. HPLC determn in human plasma: D. Hotz, E. Brode, J. Chromatogr. 277, 217 (1983). Disposition and identification of major metabolites in rats: K. Nambu et al., Arzneim.-Forsch. 38, 909 (1988).

  • Pseudoephedrine CAS Registry Number: 90-82-4 (1S,2S)-2-甲氨基-1-苯基丙-1-醇


    CAS Name: (aS)-a-[(1S)-1-(methylamino)ethyl]benzenemethanol
    Additional Names: (1S,2S)-2-methylamino-1-phenylpropan-1-ol; d-y-ephedrine; d-isoephedrine
    Percent Composition: C 72.69%, H 9.15%,...
    Literature References: Sympathomimetic amine found in plants of the genus Ephedra (Ephedraceae) known in traditional medicine as Ma Huang. a-Adrenergic agonist; (+)-threo-isomer of ephedrine, q.v. Isoln from E. vulgaris: A. Ladenburg, C. Oelschlägel, Ber. 22, 1823 (1889). Synthesis: E. Späth, R. Göhring, Monatsh. Chem. 41, 319 (1920). HPLC determn in Ma Huang: B. J. Gurley et al., J. Pharm. Sci. 87, 1547 (1998); in plasma: P. Guo et al., Biomed. Chromatogr. 13, 61 (1999). Toxicity: M. D. Fairchild, G. A. Alles, J. Pharmacol. Exp. Ther. 158, 135 (1967). Comprehensive description: S. A. Benezra, J. W. McRae, Anal. Profiles Drug Subs. 8, 489-507 (1979). Review of clinical pharmacology: D. T. D. Hughes et al., J. Clin. Hosp. Pharm. 8, 315-321 (1983). Clinical trial for prevention of otic barotrauma: J. S. Jones et al., Am. J. Emerg. Med. 16, 262 (1998); in nasal congestion: D. Taverner et al., Clin. Otolaryngol. 24, 47 (1999).

  • Procaterol CAS Registry Number: 72332-33-3 5-(1-羟基-2-异丙胺基丁基)-8-羧基喹诺酮


    CAS Name: rel-8-Hydroxy-5-[(1R,2S)-1-hydroxy-2-[(1-methylethyl)amino]butyl]-2(1H)-quinolinone
    Additional Names: (±)-erythro-8-hydroxy-5-[1-hydroxy-2-(isopropylamino)butyl]carbostyril
    Pe...
    Literature References: Sympathomimetic amine with selective b2-adrenergic agonist activity. Prepn: K. Nakagawa et al., BE 823841; eidem, US 4026897 (1975, 1977 both to Otsuka); S. Yoshizaki et al., J. Med. Chem. 19, 1138 (1976). Prepn of optical isomers: eidem, ibid. 20, 1103 (1977). Assessment of selective action: H. Himori, N. Taira, Br. J. Pharmacol. 61, 9 (1977). Metabolism: Y. Yasuda et al., Arzneim.-Forsch. 29, 261 (1979). Pharmacokinetics: M. Ishigami et al., ibid. 266. Series of reproduction studies: Iyakuhin Kenkyu 10, 68-111 (1979), C.A. 90, 197728f-30a (1979). Antigenicity test: N. Nakagiri, S. Tei, Oyo Yakuri 17, 363 (1979), C.A. 91, 186577a (1979).

  • Phenylpropanolamine CAS Registry Number: 14838-15-4


    CAS Name: (aS)-rel-a-[(1R)-1-Aminoethyl]benzenemethanol
    Additional Names: (1RS,2SR)-2-amino-1-phenyl-1-propanol; erythro-2-amino-1-phenyl-1-propanol; dl-norephedrine
    Percent Composition: C 7...
    Literature References: Sympathomimetic amine; racemic mixture of d- and l-norephedrine. Prepn: F. W. Calliess, Arch. Pharm. 250, 141 (1912); P. Rabe, Ber. 45, 2163 (1912); F. W. Hoover, H. B. Hass, J. Org. Chem. 12, 506 (1947); and prepn of enantiomers: W. N. Nagai, S. Kanao, Ann. 470, 157 (1929); C. Jarowski, W. H. Hartung, J. Org. Chem. 8, 564 (1943). Crystal structure: A. Podder et al., Indian J. Phys. 53A, 652 (1979). HPLC determn in plasma and urine: K. Yamashita et al., J. Chromatogr. 527, 103 (1990). Clinical studies of decongestant activity: O. K. Haugeto et al., J. Otolaryngol. 10, 359 (1981); M. Bende et al., Rhinology 23, 43 (1985); in stress incontinence: E. Fossberg et al., Urol. Int. 38, 293 (1983); in weight loss: D. E. Schteingart, Int. J. Obes. 16, 487 (1992). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Comprehensive description: I. Kanfer et al., Anal. Profiles Drug Subs. 12, 357-383 (1983). Review of anorexic effects: P. J. Wellman, Neurosci. Biobehav. Rev. 14, 339-355 (1990); of toxicology: R. Hanzlick, G. Davis, Am. J. Forensic Med. Pathol. 13, 37-41 (1992). Evaluation of risk of hemorrhagic stroke: W. N. Kernan et al., N. Engl. J. Med. 343, 1826 (2000).

  • Gepefrine CAS Registry Number: 18840-47-6 吉培福林


    CAS Name: 3-[(2S)-2-Aminopropyl]phenol
    Additional Names: a-methyl-m-tyramine
    Percent Composition: C 71.49%, H 8.67%, N 9.26%, O 10.58%
    Literature References: Sympathomimetic isomer of hydroxyamphetamine, q.v. Prepn: W. S. Saari et al., J. Med. Chem. 11, 1115 (1968); G. Petrik et al., DE 2712860 (1978 to Helopharm), C.A. 88, 136296a (1978). Molecular configuration and biological actions: M. L. Torchiana et al., Arch. Int. Pharmacodyn. Ther. 174, 118 (1968). In vitro study of tritium-labeled gepefrine: R. L. Dorris, Eur. J. Pharmacol. 35, 225 (1976). Biochemical-pharmacological study: R. R. Ruffolo et al., Biochem. Pharmacol. 25, 399 (1976).

  • Tixocortol CAS Registry Number: 61951-99-3 替可的松


    CAS Name: (11b)-11,17-Dihydroxy-21-mercaptopregn-4-ene-3,20-dione
    Additional Names: 11b,17a-dihydroxy-21-thio-3,20-dioxo-4-pregnene
    Percent Composition: C 66.63%, H 7.99%, O 16.91%, S 8.47%
    Literature References: Synthesis and biological activity: S. S. Simons et al., J. Steroid Biochem. 13, 311 (1980). Use in fluorescent chemoaffinity labeling: eidem, Biochemistry 18, 4915 (1979). Prepn of the 21-pivalate: D. R. Torossian et al., DE 2357778; eidem, US 4014909 (1974, 1977 both to Jouveinal). Series of articles on pharmacology, in vitro and in vivo activity of the pivalate: Arzneim.-Forsch. 31, 453-469 (1981).

  • Octanohydroxamic Acid CAS Registry Number: 7377-03-9 辛基异羟肟酸


    CAS Name: N-Hydroxyoctanamide
    Additional Names: caprylohydroxamic acid; Oct HA
    Trademarks: Taselin (Eisai)
    Percent Composition: C 60.34%, H 10.76%, N 8.80%, O 20.10%
    Literature References: Synthesis and chemical study: Inoue, Yukawa, J. Agric. Chem. Soc. Jpn. 16, 504 (1940); Ichim et al., Igiena 9, 319 (1960), C.A. 55, 16662a (1961). Activity as a urease inhibitor: Kobashi et al., Biochim. Biophys. Acta 65, 380 (1962); 227, 429 (1971); as an antimicrobial: Hase et al., Chem. Pharm. Bull. 19, 363 (1971).

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