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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

  • Avilamycin CAS Registry Number: 11051-71-1 阿维霉素

    Trademarks: Maxus (Elanco); Surmax (Elanco)
    Literature References: Polyether antibiotic complex produced by Streptomyces viridochromogenes, ETH 23575 (NRRL 2860); belongs to the orthosomycin family of antibiotics, members of which contain one or more ortho ester linkages associated with carbohydrate residues. Isoln: E. Gaeumann et al., DE 1116864; eidem, US 3131126 (1961, 1964 both to Ciba-Geigy); and characterization: F. Buzzetti et al., Experientia 24, 320 (1968). Mechanism of action studies: H. Wolf, FEBS Lett. 36, 181 (1973). Avilamycin A is the main component; avilamycins B through N are also known and are derivatives of A differing at the C-45 linkage and/or the C-56 ketone adduct. Isoln of avilamycin C: W. Heilman et al., Helv. Chim. Acta 62, 1 (1979). Structural study of A and C: eidem, ibid.; W. Keller-Schierlein et al., ibid. 7; E. Kupfer et al., ibid. 65, 3 (1982). Isoln and structure of avilamycins F through N: J. L. Mertz et al., J. Antibiot. 39, 877 (1986). GC determn of avilamycin residues in swine tissue and fluids: G. Formica, C. Giannone, J. Assoc. Off. Anal. Chem. 69, 763 (1986). Synthesis of the A-B fragment of avilamycins A and C: P. Jütten et al., Tetrahedron 43, 4133 (1987); of the disaccharide C-D fragment: J.-M. Beau et al., Tetrahedron Lett. 28, 1105 (1987). Use as a feed additive: F. Knusel et al., US 4185091 (1980 to Ciba-Geigy); in prevention of swine dysentery: E. E. Ose, US 4436734 (1984 to Lilly). Effect on feed conversion efficiency in swine: D. J. Jones et al., J. Anim. Sci. 65, 881 (1987). Metabolism in swine: J. D. Magnussen et al., J. Agric. Food Chem. 39, 306 (1991).

  • Tetronasin CAS Registry Number: 75139-06-9 乙基3-[(6-{[乙氧基(羰基)乙酰基]氨基}嘧啶-4-基)硫烷基]丙酸酯


    CAS Name: 4-Hydroxy-3-[(2S)-2-[(1S,2S,6R)-2-[(1E)-3-hydroxy-2-[(2R,3R,6S)-tetrahydro-3-methyl-6-[(1E,3S)-3-[(2R,3S,5R)-tetrahydro-5-[(1S)-1-methoxyethyl]-3-methyl-2-furanyl]-1-butenyl]-2H-pyran-2-...
    Literature References: Polyether antibiotic produced by Streptomyces longisporoflavus NCIB 11426. Possesses a biosynthetically rare acid grouping in the form of an acyl tetronic acid moiety. Isoln and use in ruminants: D. H. Davies, G. L. F. Norris, GB 2027013; eidem, US 4279894 (1980, 1981 both to ICI). Physical data and crystal structure: D. H. Davies et al., Chem. Commun. 1981, 1073. Solution conformation and cation-binding properties: J. Grandjean, P. Laszlo, Tetrahedron Lett. 24, 3319 (1983). Synthetic studies: A. M. Doherty, S. V. Ley, ibid. 27, 105 (1986). Biosynthetic studies: J. M. Bulsing et al., Chem. Commun. 1984, 1301; D. M. Doddrell et al., ibid. 1302; A. K. Demetriadou et al., ibid. 1985, 408. Antimicrobial activity: C. J. Newbold et al., Appl. Environ. Microbiol. 54, 544 (1988). Effect on gain efficiency in cattle: S. J. Bartle et al., J. Anim. Sci. 66, 1502 (1988).

  • Nigericin CAS Registry Number: 28380-24-7 尼日尼亚菌素


    Additional Names: Antibiotic K 178; antibiotic X-464; azalomycin M; helixin C; polyetherin A
    Percent Composition: C 66.27%, H 9.45%, O 24.28%
    Literature References: Polyether antibiotic which affects ion transport and ATPase activity in mitochondria; produced by Streptomyces hygroscopicus E-749 and structurally related to monensin, q.v. Isoln, characterization, production: R. L. Harned et al., Antibiot. Chemother. 1, 594 (1951); J. Berger et al., J. Am. Chem. Soc. 73, 5295 (1951); J. Shoji et al., J. Antibiot. 21, 402 (1968). Structure: L. K. Steinrauf et al., Biochem. Biophys. Res. Commun. 33, 29 (1968); T. Kubota et al., Chem. Commun. 1968, 1541; T. Kubota, S. Matsutani, J. Chem. Soc. C 1970, 695. Use in coccidiosis: M. Gorman, R. L. Hamill, US 3555150 (1971 to Lilly). Effect on calcium uptake and membrane potential in mitochondria: H. Rottenberg, A. Scarpa, Biochemistry 13, 4811 (1974). Stimulation of ATPase activity: H. Sze, Proc. Natl. Acad. Sci. USA 77, 5904 (1980). Approach to synthesis: C. P. Holmes, P. A. Bartlett, J. Org. Chem. 54, 98 (1989).

  • Monensin CAS Registry Number: 17090-79-8 莫能菌素


    CAS Name: 2-[5-Ethyltetrahydro-5-[tetrahydro-3-methyl-5-[tetrahydro-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyl-2H-pyran-2-yl]-2-furyl]-2-furyl]-9-hydroxy-b-methoxy-a,g,2,8-tetramethyl-1,6-dioxaspiro...
    Literature References: Polyether antibiotic. Major factor in antibiotic complex isolated from Streptomyces cinnamonensis. Discovery and isolation: Haney, Hoehn, Antimicrob. Agents Chemother. 1967, 349. Production: Haney, Hoehn, US 3501568 (1970 to Lilly). Structure: Agtarap et al., J. Am. Chem. Soc. 89, 5737 (1967). Crystal structure studies: Lutz et al., Helv. Chim. Acta 53, 1732 (1970); ibid. 54, 1103 (1971). Fermentation studies: Stark et al., Antimicrob. Agents Chemother. 1967, 353. Chemistry: Agtarap, Chamberlin, ibid. 359. Stereocontrolled total synthesis: T. Fukuyama et al., J. Am. Chem. Soc. 101, 262 (1979); D. B. Collum et al., ibid. 102, 2117, 2118, 2120 (1980). 13C-NMR study: J. A. Robinson, D. L. Turner, Chem. Commun. 1982, 148. Biosynthesis: Day et al., Antimicrob. Agents Chemother. 4, 410 (1973). Review: Stark, "Monensin, A New Biologically Active Compound Produced by a Fermentation Process", in Fermentation Advances, Pap. Int. Ferment. Symp., 3rd, 1968, D. Perlman, Ed. (Academic Press, New York, 1969) pp 517-540.

  • Laidlomycin CAS Registry Number: 56283-74-0 来洛霉素


    CAS Name: 16-Deethyl-3-O-demethyl-16-methyl-3-O-(1-oxopropyl)monensin
    Percent Composition: C 63.59%, H 8.94%, O 27.47%
    Literature References: Polyether ionophore antibiotic; structurally related to monensin, q.v. Isoln from Streptomyces spp. and antimicrobial activity: F. Kitame et al., J. Antibiot. 27, 884 (1974). Structure determn: F. Kitame, N. Ishida, ibid. 29, 759 (1976). Prepn of esters: A. F. Kluge, R. D. Clark, EP 24189 (1981 to Syntex). 13C-NMR study and enhancement of biological activities: R. D. Clark et al., J. Antibiot. 35, 1527 (1982). Mechanism of action study: U. Gräfe et al., J. Basic Microbiol. 29, 391 (1989). HPLC determn in fermentation broth: M. Beran et al., Chromatographia 31, 603 (1991). Effect on cattle growth: M. T. Van Koevering et al., 1991 Animal Science Research Report (Agricultural Experiment Station, Oklahoma State University, Stillwater, OK, 1991) 241; M. L. Galyean et al., J. Anim. Sci. 70, 2950 (1992).

  • Triaziquone CAS Registry Number: 68-76-8 三亚胺醌


    CAS Name: 2,3,5-Tris(1-aziridinyl)-2,5-cyclohexadiene-1,4-dione
    Additional Names: 2,3,5-tris(1-aziridinyl)-p-benzoquinone; 2,3,5-tris(aziridino)-1,4-benzoquinone; 2,3,5-tris(ethyleneimino)benzo...
    Literature References: Polyfunctional alkylating agent. Prepn: Gauss, Domagk, US 2976279 (1961 to Schenley). Review of biochemical, physiological and genetic effects: G. Obe, B. Beek, Mutat. Res. 65, 21-70 (1979); of structure and chemical reactivity: P. Rademacher, G. Obe, ibid. 340, 37-49 (1995).

  • Lichenin CAS Registry Number: 1402-10-4 地衣淀粉/地衣多糖


    Additional Names: Moss starch
    Percent Composition: C 44.45%, H 6.22%, O 49.34%
    Literature References: Polyglucan from Cetraria islandica (L.) Ach., Parmeliaceae (Iceland Moss). Isoln: Peat et al., J. Chem. Soc. 1957, 3916. Linear polysaccharide structure composed of regular sequences of two (1®4)- and one (1®3)-b-D-glucopyranosyl residues: Perlin, Suzuki, Can. J. Chem. 40, 50 (1962); Fleming, Manners, Biochem. J. 100, 4, 24 (1966). Exhibits antineoplastic activity: Shibata, JP 71 17147 (1971), C.A. 75, 67474z (1971); Tadahiro et al., Chem. Pharm. Bull. 20, 2445 (1972). NMR spectrum: D. Gagnaire, M. Vincedon, Bull. Soc. Chim. Fr. 1977, 479.

  • Discodermolide CAS Registry Number: 127943-53-7 盘皮海绵内酯


    CAS Name: (3R,4S,5R,6S)-6-[(2S,3Z,5S,6S,7S,8Z,11S,12R,13S,14S,15S,16Z)-14-[(Aminocarbonyl)oxy]-2,6,12-trihydroxy-5,7,9,11,13,15-hexamethyl-3,8,16,18-nonadecatetraenyl]tetrahydro-4-hydroxy-3,5-dime...
    Literature References: Polyhydroxylated lactone isolated from the marine sponge, Discodermia dissoluta. Naturally occurring (+)-form stabilizes microtubles and inhibits cell proliferation with the same mechanism as paclitaxel, q.v. Isoln and structure determn: S. P. Gunasekera et al., J. Org. Chem. 55, 4912 (1990); correction: ibid. 56, 1346 (1991). Total synthesis: D. T. Hung et al., J. Am. Chem. Soc. 118, 11054 (1996). Review of total syntheses: I. Paterson, G. J. Florence, Eur. J. Org. Chem. 2003, 2193-2208. Series of articles on industrial-scale synthesis: S. J. Mickel et al., Org. Process Res. Dev. 8, 92-130 (2004). NMR soln structure determn: A. B. Smith, III et al., Org. Lett. 3, 695 (2001). Mechanism of action: D. T. Hung et al., Chem. Biol. 3, 287 (1996); E. ter Haar et al., Biochemistry 35, 243 (1996). Synergistic activity with paclitaxel in cancer cells: S. Honore et al., Cancer Res. 64, 4957 (2004).

  • Ponasterone A CAS Registry Number: 13408-56-5 坡那甾酮A


    CAS Name: (2b,3b,5b,22R)-2,3,14,20,22-Pentahydroxycholest-7-en-6-one
    Additional Names: 25-deoxyecdysterone; 25-deoxy-20-hydroxyecdysone
    Percent Composition: C 69.80%, H 9.55%, O 20.66%
    Literature References: Polyhydroxylated steroid with strong moulting hormone activity; first phytoecdysteroid to be isolated. Isoln with ponasterones B, C, D, from plant source, Podocarpus nakaii Hay., Podocarpaceae and structure determn: K. Nakanishi et al., Chem. Commun. 1966, 915; isoln from various Japanese ferns: T. Takemoto et al., Chem. Pharm. Bull. 21, 2336 (1973). Isoln from crustaceans: J. F. McCarthy, Steroids 34, 799 (1979). Stereochemical elucidation: H. Moriyama, K. Nakanishi, Tetrahedron Lett. 1968, 1111; using 13C-NMR: H. Hikino et al., Chem. Pharm. Bull. 23, 125 (1975). Chromatographic sepn: M. Hori, Steroids 14, 33 (1969). HPLC analysis: I. D. Wilson et al., J. Chromatogr. 238, 97 (1982); R. E. Isaac et al., ibid. 246, 317 (1982). Synthesis: G. Hüppi, J. B. Siddall, Tetrahedron Lett. 1968, 1113. Moulting hormone activity on houseflies, silkworms: M. Kobayashi et al., Steroids 9, 529 (1967); on various insects: W. E. Robbins et al., ibid. 16, 105 (1970). Hormonal regulation to increase yield from silkworms: T. Okauchi et al., US 3941879 (1976 to Takeda). Used to characterize ecdysteroid receptors in Drosophilia cells: P. Maroy et al., Proc. Natl. Acad. Sci. USA 75, 6035 (1978); B. A. Sage et al., J. Biol. Chem. 257, 6373 (1982). Review of ponasterones: K. Nakanishi, Bull. Soc. Chim. Fr. 1969, 3475. See also Ecdysteroids.

  • Metaldehyde CAS Registry Number: 9002-91-9 多聚乙醛


    Additional Names: Metacetaldehyde
    Literature References: Polymer of acetaldehyde. (C2H4O)n. Prepd by polymerization of acetaldehyde in the presence of HCl, H2SO4 at low temp: Kekule, Zincke, Ann. 162, 125 (1872); in the presence of pyridine and HBr: R. S. Wilder, US 2426961 (1947 to Publicker Ind.). Use as molluscicide: R. M. Coloso et al., Crop Prot. 17, 669 (1998).

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