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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

  • Pyridomycin CAS Registry Number: 18791-21-4 3-羟基-N-[(2Z,5R,6S,9S,10S,11R)-10-羟基-5,11-二甲基-2-(1-甲基丙亚基)-3,7,12-三氧代-9-(3-吡啶甲基)-1,4-二氧杂-8-氮杂环十二烷-6-基]-2-吡啶甲酰胺


    CAS Name: 3-Hydroxy-N-[(2Z,5R,6S,9S,10S,11R)-10-hydroxy-5,11-dimethyl-2-(1-methylpropylidene)-3,7,12-trioxo-9-(3-pyridinylmethyl)-1,4-dioxa-8-azacyclododec-6-yl]-2-pyridinecarboxamide
    Percent C...
    Literature References: Antimycobacterial antibiotic substance produced by Streptomyces albidofuscus Okami et Umezawa, nov sp., renamed S. pyridomyceticus. Isoln: Maeda et al., J. Antibiot. 6A, 140 (1953); K. Yagishita, ibid. 7A, 143 (1954). Degradation studies: Maeda, ibid. 10A, 94 (1957). Structure: Koyama et al., Tetrahedron Lett. 1967, 3587; H. Ogawara et al., Chem. Pharm. Bull. 16, 679 (1968). Synthetic study: M. Kinoshita, M. Awamura, Bull. Chem. Soc. Jpn. 51, 869 (1978); M. Kinoshita et al., ibid. 3595. Production: JP 54 7048; JP 55 1349; JP 56 9566 (1954, 1955, 1956 all to Nippon Antibiotic Subst. Sci. Assoc.).

  • Bifonazole CAS Registry Number: 60628-96-8 联苯苄唑


    CAS Name: 1-([1,1'-Biphenyl]-4-ylphenylmethyl)-1H-imidazole
    Additional Names: (±)-1-(p,a-diphenylbenzyl)imidazoleTrademarks: Amycor (Lipha); Azolmen (Menarini); Bedriol (Andromaco); Mycosp...
    Literature References: Antimycotic deriv of imidazole. Prepn: E. Regel et al., DE 2461406; eidem, US 4118487 (1976, 1978 both to Bayer). Series of articles on in vitro and in vivo antimycotic efficacy, microscopic studies, pharmacokinetics, efficacy in dermatomycoses and comparison with clotrimazole and miconazole, q.q.v.: Arzneim.-Forsch. 33, 517-551, 745-754 (1983). Toxicology: G. Schlüter, ibid. 739.

  • Amorolfine CAS Registry Number: 78613-35-1 阿莫罗芬


    CAS Name: cis-4-[3-[4-(1,1-Dimethylpropyl)phenyl]-2-methylpropyl]-2,6-dimethylmorpholine
    Additional Names: cis-4-[3-(4-tert-amylphenyl)-2-methylpropyl]-2,6-dimethylmorpholine; (±)-cis-2,6-...
    Literature References: Antimycotic morpholine derivative; inhibits fungal ergosterol biosynthesis. Prepn (unspec stereochem): A. Pfiffner, K. Bohnen, DE 2752096; A. Pfiffner, US 4202894 (1978, 1980 both to Hoffmann-La Roche); of cis-form: NL 8004537 (1980 to Hoffmann-La Roche). In vitro comparative antifungal spectrum: S. Shadomy et al., Sabouraudia 22, 7 (1984). Mechanism of action: A. Polak-Wyss et al., ibid. 23, 433 (1985); A. Polak, Ann. N.Y. Acad. Sci. 544, 221 (1988). LC determn in pharmaceutical formulations: M. A. Czech et al., J. Pharm. Biomed. Anal. 9, 1019 (1991). Series of articles on mode of action and clinical trials: Clin. Exp. Dermatol. 17, Suppl. 1, 1-70 (1992). Review of pharmacology and clinical efficacy: M. Haria, H. M. Bryson, Drugs 49, 103-120 (1995).

  • Cervicarcin CAS Registry Number: 18700-78-2


    CAS Name: 1,2,3,4-Tetrahydro-1,3,4,5,10-pentahydroxy-2-methyl-3-[(3-methyloxiranyl)carbonyl]-4a,9a-epoxyanthracen-9(10H)-one
    Additional Names: 4a,9a-epoxy-3-(2,3-epoxybutyryl)-1,2,3,4,4a,9a-hex...
    Literature References: Antineoplastic antibiotic produced by Streptomyces ogaensis: Okuma et al., J. Antibiot. 15A, 152, 247 (1962). Prepn: Sumiki et al., JP 64 7400 (1964 to Inst. Phys. Chem. Res.). Structure: Marumo et al., J. Am. Chem. Soc. 86, 4507 (1964); eidem, Agric. Biol. Chem. 32, 209 (1968). Stereochemistry: eidem, ibid. 35, 1931 (1971). Activity studies: C. Itakura et al., J. Antibiot. 16A, 231 (1963).

  • Primocarcin CAS Registry Number: 3750-26-3 5-乙酰氨基-4-氧代己-5-烯酰胺


    CAS Name: 5-(Acetylamino)-4-oxo-5-hexenamide
    Additional Names: 4-acetamido-4-penten-3-one-1-carboxamide
    Percent Composition: C 52.17%, H 6.57%, N 15.21%, O 26.06%
    Literature References: Antineoplastic antibiotic produced by the actinomycete, Nocardia fukaya. Isoln: Y. Sumiki et al., J. Antibiot. 13A, 416 (1960); Isono, Suzuki, ibid. 15A, 77 (1962). Isoln from Streptomyces diastatochromogens var. luteus: H. Abe et al., ibid. 20A, 167 (1967). Structure: Isono, ibid. 15A, 80 (1962). Synthesis: Bowman et al., J. Chem. Soc. 1965, 470.

  • Selamectin CAS Registry Number: 220119-17-5 司拉克丁


    CAS Name: (5Z)-25-Cyclohexyl-4'-O-de(2,6-dideoxy-3-O-methyl-a-L-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)avermectin A1a
    Additional Names: 5-oxoimin...
    Literature References: Antiparasitic semisynthetic avermectin, q.v. Prepn: B. F. Bishop et al., WO 9415944; eidem, US 5981500 (1994, 1999 both to Pfizer).

  • Seocalcitol CAS Registry Number: 134404-52-7 西奥骨化醇


    CAS Name: (1R,3S,5Z)-5-[(2E)-[(1R,3aS,7aR)-1-[(lR,2E,4E)-6-Ethyl-6-hydroxy-1-methyl-2,4-octadienyl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-1,3-cyclohexanediol
    Additional ...
    Literature References: Antiproliferative vitamin D analog with reduced effects on calcium metabolism. Prepn: E. Binderup, M. J. Calverley, WO 9100855; US 5190935 (1991, 1993 both to Leo Pharm.). LC-MS-MS determn in serum: A.-M. Kissmeyer et al., J. Chromatogr. B 740, 117 (2000). Pharmacokinetics and metabolism: A.-M. Kissmeyer, J. T. Mortensen, Xenobiotica 30, 815 (2000). Mechanism of action study: G. A. DeMasters et al., J. Steroid Biochem. Mol. Biol. 92, 365 (2004). Clinical evaluation in pancreatic cancer: T. R. J. Evans et al., Br. J. Cancer 86, 680 (2002); in hepatocellular carcinoma: K. Dalhoff et al., Br. J. Cancer 89, 252 (2003). Review of pharmacology and clinical experience: C. M. Hansen et al., Curr. Pharm. Des. 6, 803-828 (2000).

  • Gymnemic Acid CAS Registry Number: 1399-64-0


    Additional Names: Gymnemin
    Literature References: Antisaccharin principle occurring in the leaves of Gymnema sylvestre R. Br. and allied Asclepiadaceae: Hooper, Chem. News 59, 159 (1889); Mhaskar, Caius, Indian J. Med. Res. No. 16, 1 (1930); Warren, Pfaffman, J. Appl. Physiol. 14, 40 (1959); Stöcklin et al., Helv. Chim. Acta 50, 474 (1967). A complex mixture of at least nine closely related acidic glycosides, the major active component being gymnemic acid A1: Stöcklin, J. Agric. Food Chem. 17, 704 (1969); Dateo, Long, ibid. 21, 899 (1973). Separation of major components: Sinsheimer et al., J. Pharm. Sci. 59, 622, 629 (1970). Completely obtunds taste for several hours for sweet but not for bitter, sour, or salty substances: G. Hellekant et al., Acta Physiol. Scand. 124, 399 (1985).

  • Racecadotril CAS Registry Number: 81110-73-8 消旋卡多曲


    CAS Name: N-[2-[(Acetylthio)methyl]-1-oxo-3-phenylpropyl]glycine phenylmethyl ester
    Additional Names: N-[(R,S)-3-acetylthio-2-benzylpropanoyl]glycine benzyl ester; acetorphan
    Trademarks: Hid...
    Literature References: Antisecretory enkephalinase inhibitor. Prepn: B. Roques et al., EP 38758 (1981); eidem, US 4513009 (1985 to Bioprojet). Pharmacology: J.-M. Lecomte et al., J. Pharmacol. Exp. Ther. 237, 937 (1986). Effect on intestinal transit: J. F. Bergmann et al., Aliment. Pharmacol. Ther. 6, 305 (1992). Clinical trial in acute diarrhea: P. Baumer et al., Gut 33, 753 (1992); in children: E. Salazar-Lindo et al., N. Engl. J. Med. 343, 463 (2000). Symposium on pharmacology and clinical experience: Aliment. Pharmacol. Ther. 13, Suppl. 6, 1-32 (1999). Review of clinical development: J.-C. Schwartz, Int. J. Antimicrob. Agents 14, 75-79 (2000); J. M. Lecomte, ibid. 81-87.

  • Arbaprostil CAS Registry Number: 55028-70-1 15(R)-15-甲基前列腺素E2


    CAS Name: (5Z,11a,13E,15R)-11,15-Dihydroxy-15-methyl-9-oxoprosta-5,13-dien-1-oic acid
    Additional Names: (15R)-15-methylprostaglandin E2; (15R)-15-methyl-PGE2; (E,Z)-(1R,2R,3R)-7-[3-hydroxy-2-[(...
    Literature References: Antisecretory, cytoprotective derivative of prostaglandin E2, q.v. Prepn: G. L. Bundy et al., DE 2121980; G. L. Bundy, US 3804889 (1971, 1974 both to Upjohn). Synthetic studies: G. Bundy et al., Ann. N.Y. Acad. Sci. 180, 76 (1971); E. W. Yankee, G. Bundy, J. Am. Chem. Soc. 94, 3651 (1972). Synthesis of R- and S-methyl esters: E. W. Yankee et al., ibid. 96, 5865 (1974). HPLC separation of epimers: R. K. Lustgarten, J. Pharm. Sci. 65, 1533 (1976); G. E. Peng, V. K. Sood, J. Liq. Chromatogr. 6, 1499 (1983). Pharmacology: J. R. Weeks et al., J. Pharmacol. Exp. Ther. 186, 67 (1973). Comparative activity of epimers: A. Robert, E. W. Yankee, Proc. Soc. Exp. Biol. Med. 148, 1155 (1975). Kinetics of epimerization: M. V. Merritt, G. E. Bronson, J. Am. Chem. Soc. 100, 1891 (1978). Clinical study in duodenal ulcers: G. Vantrappen et al., Gastroenterology 83, 357 (1982); in prevention of aspirin-induced gastric mucosal injury: D. A. Gilbert et al., ibid. 86, 339 (1984).

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