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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

  • Dehydroemetine CAS Registry Number: 4914-30-1 去氢依米丁


    CAS Name: 2,3-Didehydro-6',7',10,11-tetramethoxyemetan
    Additional Names: 2,3-dehydroemetine; 2-dehydroemetine
    Percent Composition: C 72.77%, H 8.00%, N 5.85%, O 13.37%
    Literature References: Synthetic analog of emetine, q.v.; the (-)-form is therapeutically active. Synthesis of racemic 2,3-dehydroemetine: Brossi et al., Helv. Chim. Acta 42, 772 (1959). Stereospecific synthesis of (±)-form and (±)-2,3-dehydroisoemetine, the (1¢b)-isomer: Clark et al., J. Chem. Soc. 1962, 2479. Separation of the four possible isomers: Brossi, Burkhardt, Experientia 18, 211 (1962). Absolute configuration and bioactivity of isomers: A. Brossi et al., Helv. Chim. Acta 45, 2219 (1962). Prepn of pure (-)-form: A. Brossi, BE 629898; eidem, US 3311633 (1963, 1967 both to Hoffmann-La Roche); N. Whittaker J. Chem. Soc. C 1969, 94. Antiprotozoal activity in vitro: G. H. Al-Khateeb et al., Chemotherapy (Basel) 23, 267 (1977). Review of use in amebiasis: G. Woolfe, Prog. Drug Res. 8, 12 (1965).

  • Treprostinil CAS Registry Number: 81846-19-7 曲前列尼尔


    CAS Name: [[(1R,2R,3aS,9aS)-2,3,3a,4,9,9a-Hexahydro-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl]oxy]acetic acid
    Additional Names: 9-deoxy-2',9a-methano-3-oxa-4,5,6-trinor-3,7-(1',3'-...
    Literature References: Synthetic analog of prostacyclin, q.v. Prepn: P. A. Aristoff et al., GB 2070596; idem, US 4306075 (both 1981 to Upjohn). Pharmacology: R. P. Steffen, M. de la Mata, Prostaglandins Leukotrienes Essen. Fatty Acids 43, 277 (1991). Pharmacokinetics: M. J. McNulty et al., ibid. 159; of intravenous and subcutaneous administration: K. Laliberte et al., J. Cardiovasc. Pharmacol. 44, 209 (2004). RIA determn in plasma: J. W. A. Findlay et al., ibid. 167. Clinical study in pulmonary arterial hypertension: G. Simonneau et al., Am. J. Respir. Crit. Care Med. 165, 800 (2002); by s. c. infusion: R. J. Oudiz et al., Chest 126, 420 (2004); by continuous i.v.: V. F. Tapson et al., ibid. 129, 683 (2006).

  • Fenprostalene CAS Registry Number: 69381-94-8 芬前列林


    CAS Name: (4S)-rel-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-[(1E,3R)-3-hydroxy-4-phenoxy-1-butenyl]cyclopentyl]-4,5-heptadienoic acid methyl ester
    Additional Names: (±)-9a,11a,15a-trihydroxy-16-ph...
    Literature References: Synthetic analog of prostaglandin F2a, related structurally to prostalene, q.v. Prepn: J. M. Muchowski, J. H. Fried, US 3985791; A. R. Van Horn et al., US 4178457 (1976, 1979 both to Syntex). Effect on pregnancy in beagles: B. Vickery, G. McRae, Biol. Reprod. 22, 438 (1980). Duration of action study: B. H. Vickery et al., Prostaglandins Med. 5, 93 (1980).

  • Ganaxolone CAS Registry Number: 38398-32-2 加奈索酮


    CAS Name: (3a,5a)-3-Hydroxy-3-methylpregnan-20-onePercent Composition: C 79.46%, H 10.91%, O 9.62%
    Literature References: Synthetic analog of the neuroactive steroids known as epalons that allosterically modulate the g-aminobutyric acid type A (GABAA) receptor. Prepn: M. C. Cook et al., DE 2162555; eidem, US 3953429 (1972, 1976 both to Glaxo); D. J. Hogenkamp et al., J. Med. Chem. 40, 61 (1997). Binding study and anticonvulsant activity: R. B. Carter et al., J. Pharmacol. Exp. Ther. 280, 1284 (1997). Clinical pharmacology: E. P. Monaghan et al., Epilepsia 38, 1026 (1997). Determn in serum by HPLC-MS-MS: K. Ramu et al., J. Chromatogr. B 751, 49 (2001).

  • Desmopressin CAS Registry Number: 16679-58-6 去氨加压素


    CAS Name: 1-(3-Mercaptopropanoic acid)-8-D-arginine vasopressin
    Additional Names: 8-D-arginine-1-(3-mercaptopropanoic acid) vasopressin; 1-desamino-8-D-arginine vasopressin
    Percent Compositi...
    Literature References: Synthetic analog of vasopressin, q.v., with antidiuretic activity and decreased pressor effects. Improves hemostasis by increasing plasma levels of von Willebrand factor, factor VIII and tissue plasminogen activator, q.q.v. Prepn: M. Zaoral et al., FR 1540536; eidem, US 3497491 (1968, 1970 both to Ceskoslovenska Akad. Ved). Syntheses: R. L. Huguenin, R. A. Boissonnas, Helv. Chim. Acta 49, 695 (1966); M. Zaoral et al., Collect. Czech. Chem. Commun. 32, 1250 (1967). Review of clinical experience in bleeding disorders: P. M. Mannucci, Blood 90, 2515-2521 (1997); in treatment of nocturnal enuresis: P. E. V. van Kerrebroeck, BJU Int. 89, 420-425 (2002); of mechanism of hemostatic effects: J. E. Kaufmann, U. M. Vischer, J. Thromb. Haemostasis 1, 682-689 (2003).

  • Calusterone CAS Registry Number: 17021-26-0 卡普睾酮


    CAS Name: (7b,17b)-17-Hydroxy-7,17-dimethylandrost-4-en-3-one
    Additional Names: 7b,17a-dimethyltestosterone; methosarbPercent Composition: C 79.70%, H 10.19%, O 10.11%
    Literature References: Synthetic androgen epimeric with bolasterone, q.v. Has been used in treatment of breast cancer. Prepn: Campbell, Babcock, US 3029263; US 3341557 (1962, 1967 both to Upjohn). Clinical studies: Gordan et al., J. Am. Med. Assoc. 219, 483 (1972).

  • Amrubicin CAS Registry Number: 110267-81-7 氨柔比星


    CAS Name: (7S,9S)-9-Acetyl-9-amino-7-[(2-deoxy-b-D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-naphthacenedione
    Additional Names: (+)-9-amino-4-demethoxy-9-deoxy-7-O-(2-...
    Literature References: Synthetic anthracycline antibiotic; inhibits DNA topoisomerase II. Prepn: K. Ishizumi et al., EP 107486; eidem, US 4673668 (1984, 1987 both to Sumitomo); eidem, J. Org. Chem. 52, 4477 (1987). NMR study of complex with DNA: J. Igarashi, M. Sunagawa, Bioorg. Med. Chem. Lett. 5, 2923 (1995). Mechanism of action: M. Hanada et al., Jpn. J. Cancer Res. 89, 1229 (1998). Toxicology: S. Morisada et al., ibid. 80, 77 (1989). Clinical pharmacokinetics: K. Inoue et al., Invest. New Drugs 7, 213 (1989); Y. Matsunaga et al., Ther. Drug Monit. 28, 76 (2006). Clinical evaluation in lung cancer: T. Sugiura et al., Invest. New Drugs 23, 331 (2005); in combination with cisplatin: Y. Ohe et al., Ann. Oncol. 16, 430 (2005).

  • Carbetocin CAS Registry Number: 37025-55-1 醋酸卡贝缩宫素


    CAS Name: 1-Butanoic acid-2-(O-methyl-L-tyrosine)-1-carbaoxytocin
    Additional Names: 1-butyric acid-2-[3-(p-methoxyphenyl)-L-alanine]oxytocin; deamino-2-O-methyltyrosine-1-carbaoxytocin; 1-thia-...
    Literature References: Synthetic carba-analog of oxytocin, q.v. Prepn: I. Fric et al., Collect. Czech. Chem. Commun. 39, 1290 (1974); J. H. Cort et al., DE 2732175 (1976 to Czech. Akad. Ved.). Chromatographic properties: M. Lebl, Collect. Czech. Chem. Commun. 45, 2927 (1980). Uterotonic and galactogogic activity: T. Barth et al., ibid. 3045; T. Barth et al., ibid. 46, 2441 (1981). Pharmacokinetics in lactating sows: N. Cort et al., Am. J. Vet. Res. 42, 1804 (1981). Use in regulation of bovine labor: Z. Veznik et al., ibid. 40, 425 (1979). Effect on milk let-down in sows: N. Cort et al., ibid. 43, 1283 (1982).

  • Prednisolone CAS Registry Number: 50-24-8 泼尼松龙


    CAS Name: (11b)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione
    Additional Names: 1,4-pregnadiene-3,20-dione-11b,17a,21-triol; 1,4-pregnadiene-11b,17a,21-triol-3,20-dione; 3,20-dioxo-11b,17a,21-...
    Literature References: Synthetic corticosteroid; metabolically interconvertible with prednisone, q.v. Prepn: A. Nobile et al., J. Am. Chem. Soc. 77, 4184 (1955); A. Nobile, US 2837464; US 3134718 (1958, 1964, both to Schering); Herzog et al., Tetrahedron 18, 581 (1962). HPLC determn in urine: B. M. Frey, F. J. Frey, J. Chromatogr. 229, 283 (1982). Clinical use in advanced cancer: R. G. Twycross, D. Guppy, Practitioner 229, 57 (1985); in inflammatory bowel disease: C. J. Hawkey, Neth. J. Med. 35 Suppl 1, S21-S26 (1989). Review of clinical pharmacology: W. J. Jusko, J. Q. Rose, Ther. Drug Monit. 2, 169-176 (1980); of pharmacokinetics and metabolism: B. M. Frey, F. J. Frey, Clin. Pharmacokinet. 19, 126-146 (1990). Comprehensive description: S. L. Ali, Anal. Profiles Drug Subs. Excip. 21, 415-500 (1992).

  • Vindesine CAS Registry Number: 53643-48-4 长春地辛


    CAS Name: 3-(Aminocarbonyl)-O4-deacetyl-3-de(methoxycarbonyl)vincaleukoblastine
    Additional Names: desacetylvinblastine amide; VDSPercent Composition: C 68.50%, H 7.35%, N 9.29%, O 14.85%
    Literature References: Synthetic deriv of the dimeric Catharanthus alkaloid vinblastine, q.v. Prepn: G. J. Cullinan, K. Gerzon, DE 2415980 (1974 to Lilly), C.A. 82, 72191r (1975); see also C. J. Burnett et al., J. Med. Chem. 21, 88 (1978). 13C-NMR spectroscopy: D. E. Dorman, J. W. Paschal, Org. Magn. Reson. 8, 413 (1976). Antitumor activity in rodents: M. J. Sweeney et al., Cancer Res. 38, 2886 (1978). Pharmacokinetics: R. J. Owellen et al., ibid. 37, 2603 (1977). Use in acute lymphocytic leukemia of childhood: W. Krivit et al., Cancer Chemother. Pharmacol. 2, 267 (1979). Brief review of preclinical and early clinical data: R. W. Dyke et al., ibid. 229. Toxicology: G. C. Todd et al., Toxicol. Environ. Health 1, 843 (1976); R. J. Owellen et al., Biochem. Pharmacol. 26, 1213 (1977).

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