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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

  • Nidulin CAS Registry Number: 10089-10-8 6-[(2E)-2-丁烯-2-基]-2,4,7-三氯-3-羟基-8-甲氧基-1,9-二甲基-11H-二苯并[b,e][1,4]二氧杂卓-11-酮


    CAS Name: (E)-2,4,7-Trichloro-3-hydroxy-8-methoxy-1,9-dimethyl-6-(1-methyl-1-propenyl)-11H-dibenzo[b,e][1,4]dioxepin-11-one
    Additional Names: methylustin; ustin methyl ether
    Percent Composit...
    Literature References: Antibiotic substance produced by a strain of Aspergillus nidulans (Eidam) Wint.: Dean et al., Nature 172, 344 (1953); Dean et al., J. Chem. Soc. 1954, 1432. Structure: Dean et al., ibid. 1960, 4829; Bycroft et al., ibid. 1963, 5148.

  • Methymycin CAS Registry Number: 497-72-3 (2R,3S,7R,9S,10S,11R)-10-[(2S,3R,4S,6R)-4-二甲基氨基-3-羟基-6-甲基-四氢吡喃-2-基]氧基-2-乙基-3-羟基-3,7,9,11-四甲基-1-氧杂环十二碳-4-烯-6,12-二酮


    Percent Composition: C 63.94%, H 9.23%, N 2.98%, O 23.85%
    Literature References: Antibiotic substance produced by a streptomycete from soil near Oswego, N.Y. Has a macrolide structure (12-membered lactone ring, compare Picromycin). Isoln and antibacterial activity: Donin et al., Antibiot. Annu. 1, 179 (1953-4). Production using Streptomyces venezuelae cultures: Dutcher et al., US 2916483 (1959 to Olin Mathieson). Structure: C. Djerassi, J. A. Zderic, J. Am. Chem. Soc. 78, 6390 (1956). Absolute configuration: Rickards, Smith, Tetrahedron Lett. 1970, 1025; Manwaring et al., ibid. 1029. Biosynthesis: Birch et al., J. Chem. Soc. 1964, 5274. Synthesis: Masamune et al., J. Am. Chem. Soc. 97, 3512 (1975). Possible mechanism of action: Wilhelm et al., Antimicrob. Agents Chemother. 1967, 236.

  • Amidomycin CAS Registry Number: 552-33-0


    Percent Composition: C 60.28%, H 8.60%, N 7.03%, O 24.09%
    Literature References: Antibiotic substance produced by an unidentified Streptomyces culture (PRL 1642). Composed of 4 moles each of D-(-)-valine and D-(-)-a-hydroxyisovaleric acid, linked alternately by ester and amide bonds to form a 24-membered ring: Vining, Taber, Can. J. Chem. 35, 1109 (1957). Structure studies: Shemyakin et al., Tetrahedron Lett. 1963, 351, Tetrahedron 19, 995 (1963).

  • Azomycin CAS Registry Number: 527-73-1 2-硝基咪唑


    CAS Name: 2-Nitro-1H-imidazole
    Percent Composition: C 31.87%, H 2.67%, N 37.16%, O 28.30%
    Literature References: Antibiotic substance produced by an unidentified Streptomyces sp. (resembling Nocardia mesenterica in some aspects) from soil collected at Shiba Shirokane Daimachi (Japan): Maeda et al., J. Antibiot. 6A, 182 (1953); Okami et al., ibid. 7A, 53 (1954); Nakamura, Umezawa, ibid. 8A, 66 (1955). Structure: Nakamura, Pharm. Bull. 3, 379 (1955). Synthesis: Beaman et al., J. Am. Chem. Soc. 87, 389 (1965); Lancini, Lazzari, Experientia 21, 83 (1965).

  • Fumagillin CAS Registry Number: 23110-15-8 夫马洁林


    CAS Name: (2E,4E,6E,8E)-2,4,6,8-Decatetraenedioic acid mono[(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1-oxaspiro[2.5]oct-6-yl] ester
    Additional Names: 2,4,6,8-...
    Literature References: Antibiotic substance produced by Aspergillus fumigatus: T. E. Eble, F. R. Hanson, Antibiot. Chemother. 1, 55 (1951); F. R. Hanson, T. E. Eble, US 2652356 (1953 to Upjohn). Purification: D. S. Tarbell et al., J. Am. Chem. Soc. 77, 5613 (1955). Structure: eidem, ibid. 82, 1005 (1960); 83, 3096 (1961). Stereochemistry: N. J. McCorkindale, J. G. Sime, Proc. Chem. Soc. London 1961, 331; J. R. Turner, D. S. Tarbell, Proc. Natl. Acad. Sci. USA 48, 733 (1962). Biosynthesis: A. J. Birch, S. F. Hussain, J. Chem. Soc. C 1969, 1473. Total synthesis of (±)-form: E. J. Corey, B. B. Snider, J. Am. Chem. Soc. 94, 2549 (1972). Anti-amebic activity: M. C. McCowen et al., Science 113, 202 (1951). Acute toxicity: J. A. DiPaolo et al., Antibiot. Annu. 1958-1959, 541. HPLC determn in trout muscle: J. Guyonnet et al., J. Chromatogr. B 666, 354 (1995). Field trial in honey bees: T. C. Webster, J. Econ. Entomol. 87, 601 (1994); in rainbow trout: R. le Gouvello et al., Aquaculture 171, 27 (1999). Clinical evaluation in intestinal microsporidiosis in immunocompromised patients: J.-M. Molina et al., N. Engl. J. Med. 346, 1963 (2002).

  • Nornidulin CAS Registry Number: 33403-37-1 6-(2-丁烯-2-基)-2,4,7-三氯-3,8-二羟基-1,9-二甲基-11H-二苯并[b,e][1,4]二氧杂卓-11-酮


    CAS Name: 2,4,7-Trichloro-3,8-dihydroxy-1,9-dimethyl-6-(1-methyl-1-propenyl)-11H-dibenzo[b,e][1,4]dioxepin-11-one
    Trademarks: Ustin
    Percent Composition: C 53.11%, H 3.52%, Cl 24.75%, O 18.62...
    Literature References: Antibiotic substance produced by Aspergillus ustus: Kurung, Science 102, 11 (1945); Hogeboom, Craig, J. Biol. Chem. 162, 363 (1946); Doering et al., J. Am. Chem. Soc. 68, 725 (1946). Structure: Dean et al., J. Chem. Soc. 1960, 4829; Bycroft et al., ibid. 1963, 5148.

  • Bacimethrin CAS Registry Number: 3690-12-8 4-氨基-2-甲氧基-5-嘧啶甲醇


    CAS Name: 4-Amino-2-methoxy-5-pyrimidinemethanol
    Additional Names: 4-amino-5-hydroxymethyl-2-methoxypyrimidine
    Percent Composition: C 46.45%, H 5.85%, N 27.08%, O 20.62%
    Literature References: Antibiotic substance produced by Bacillus megatherium from Japanese soil. Isoln and structure: F. Tanaka et al., J. Antibiot. 14A, 161 (1961); 15A, 191, 197 (1962). Prepn: GB 884772 (1961 to Merck Co.); Koppel et al., J. Org. Chem. 27, 1492, 3614 (1962). Biological studies: T. Nishimura, N. Tanaka, J. Antibiot. 16A, 179 (1963).

  • Penicillin N CAS Registry Number: 525-94-0 阿地西林


    CAS Name: (2S,5R,6R)-6-[[(5R)-5-Amino-5-carboxy-1-oxopentyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
    Additional Names: 6-(D-5-amino-5-carboxyvaleramido)-3,3...
    Literature References: Antibiotic substance produced by Cephalosporium spp found in sewage outpours: Gottshall et al., Proc. Soc. Exp. Biol. Med. 76, 307 (1951); Abraham et al., Nature 171, 343 (1953); 176, 551 (1955). Produced also by Paecilomyces persicimus: Pisano et al., Antimicrob. Agents Annu. 1960 (Plenum Press, New York, 1961) pp 41, 48; by Penicillium chrysogenum: Flynn et al., J. Am. Chem. Soc. 84, 4594 (1962). Structure: Abraham, Newton, Biochem. J. 58, 103 (1954). Production: Miller et al., US 2831797 (1958). Purification: Goodall, Sutcliffe, US 2899425 (1959 to ICI).

  • Bostrycoidin CAS Registry Number: 4589-33-7 葡萄孢镰菌素


    CAS Name: 6,9-Dihydroxy-7-methoxy-3-methylbenz[g]isoquinoline-5,10-dione
    Additional Names: 5,8-dihydroxy-6-methoxy-3-methyl-2-aza-9,10-anthraquinone
    Percent Composition: C 63.16%, H 3.89%, N...
    Literature References: Antibiotic substance produced by Fusarium bostrycoides: Hamilton et al., Antibiot. Chemother. 3, 853 (1953); Cajori et al., J. Biol. Chem. 208, 107 (1954). Structure: Arsenault, Tetrahedron Lett. 1965, 4033. Synthesis: D. W. Cameron et al., ibid. 21, 5089 (1980).

  • Javanicin CAS Registry Number: 476-45-9 爪哇梭黴素


    CAS Name: 5,8-Dihydroxy-6-methoxy-2-methyl-3-(2-oxopropyl)-1,4-naphthalenedione
    Additional Names: 3-acetonyl-5,8-dihydroxy-6-methoxy-2-methyl-1,4-naphthoquinone
    Percent Composition: C 62.07%...
    Literature References: Antibiotic substance produced by Fusarium javanicum: Arnstein, Cook, J. Chem. Soc. 1947, 1021. Prepd by reduction of fusarubin: Ruelius, Gauhe, Ann. 569, 38 (1950). Structure: Birch, Donovan, Chem. Ind. (London) 1954, 1047; Whalley, ibid. 1958, 131; Hardegger et al., Helv. Chim. Acta 47, 2027 (1964).

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