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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

  • Actinorhodine CAS Registry Number: 1397-77-9 [8,8'-Bi-1H-萘[2,3-c]吡喃]-3,3'-二乙酸,3,3',4,4',5,5',10,10'-八氢-6,6',9,9'-四羟基-1,1'-二甲基-5,5',10,10'-四甲氧基-,(1R,1'R,3S,3'S)-


    Percent Composition: C 60.57%, H 4.13%, O 35.30%
    Literature References: Antibiotic pigment produced by Streptomyces coelicolor, found in woods near Göttingen, Germany: Brockmann, Pini, Naturwissenschaften 34, 190 (1947); Brockmann et al., Ber. 83, 161 (1950). Tentative structure: Brockmann, Hieronymus, Ber. 88, 1379 (1955); Brockmann et al., Naturwissenschaften 49, 131 (1962). Structure: Brockmann, Angew. Chem. 76, 863 (1964); Brockmann et al., Ann. 698, 209 (1966). Stereochemistry: Zeeck, Christiansen, Ann. 724, 172 (1969). Biosynthesis and determn of point of dimerization: C. P. Gorst-Allman et al., J. Org. Chem. 46, 455 (1981).

  • Lactaroviolin CAS Registry Number: 85-33-6 乳菇紫素


    CAS Name: 4-Methyl-7-(1-methylethenyl)-1-azulenecarboxaldehyde
    Additional Names: 7-isopropenyl-4-methyl-1-azulenecarboxaldehyde; 1-formyl-4-methyl-7-isopropenylazulene
    Percent Composition: C...
    Literature References: Antibiotic pigment produced by the fungus Lactarius deliciosus: Willstaedt, Ber. 68, 333 (1935); 69, 997 (1936); Benesová et al., Chem. Listy 48, 882 (1954). Structure: Plattner et al., Chem. Ind. (London) 1954, 1202; Sorm et al., ibid. 1511; Heilbron, Schmid, Helv. Chim. Acta 37, 2018 (1954).

  • Boromycin CAS Registry Number: 34524-20-4


    Percent Composition: C 61.43%, H 8.48%, B 1.23%, N 1.59%, O 27.28%
    Literature References: Antibiotic produced by Streptomyces antibioticus ETH 28829: Hütter et al., Helv. Chim. Acta 50, 1533 (1967). The first known natural product in which boron has been found. It is a complex of boric acid with a tetradentate organic complexing agent and yields D-valine, boric acid and a polyhydroxy macrolide-type compound upon hydrolysis. Structure: Dunitz et al., ibid. 54, 1709 (1971). Mechanism of action studies: Pache, Zähner, Arch. Mikrobiol. 67, 156 (1969). Activity as a coccidiostat: Miller, Burg, US 3864479 (1975 to Merck Co.). Biosynthesis: T. S. S. Chen et al., J. Org. Chem. 46, 2661 (1981). Partial synthesis: M. A. Avery et al., Tetrahedron Lett. 22, 3123 (1981). Synthesis of C-3¢ to C-17¢: S. Hanessian et al., J. Am. Chem. Soc. 103, 6243 (1981); of C-3 to C-17: eidem, Can. J. Chem. 61, 634 (1983); of C-1 to C-17: J. D. White et al., J. Am. Chem. Soc. 105, 6517 (1983). Total synthesis: eidem, ibid. 111, 790 (1989). Review: Pache in Antibiotics vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (Springer-Verlag, New York, 1975) pp 585-587.

  • Frenolicin CAS Registry Number: 10023-07-1 4a,10a-环氧-1H-石脑石脑[2,3-c]吡喃-3-醋酸,3,4,5,10-四氢-9-羟基-5,10-二氧基-1-丙基,(1R,3S,4aS,10aR)-


    CAS Name: [1R-(1a,3b,4ab,10ab)]-3,4,5,10-Tetrahydro-9-hydroxy-5,10-dioxo-1-propyl-4a,10a-epoxy-1H-naphtho[2,3-c]pyran-3-acetic acid
    Percent Composition: C 62.42%, H 5.24%, O 32.34%
    Literature References: Antibiotic produced by Streptomyces fradiae: Van Meter et al., Antimicrob. Agents Annu. 1960, 77. Structure: Ellestad et al., J. Am. Chem. Soc. 88, 4109 (1966); 90, 1325 (1968). Total synthesis: A. Ichihara et al., Tetrahedron Lett. 21, 4469 (1980).

  • Aurodox CAS Registry Number: 12704-90-4 奥罗多克斯


    CAS Name: 1-Methylmocimycin
    Additional Names: antibiotic X-5108; goldinodox; goldinomycinPercent Composition: C 65.17%, H 7.71%, N 3.45%, O 23.67%
    Literature References: Antibiotic produced by Streptomyces goldiniensis var. goldiniensis: J. Berger, DE 2140322; idem, US 3708577 (1972, 1973 both to Hoffmann-La Roche). Isoln, production, properties and toxicity data: J. Berger et al., J. Antibiot. 26, 15 (1973). Improved production: J. Unowsky, D. C. Hoppe, ibid. 31, 662 (1978). Structure: H. Maehr et al., J. Am. Chem. Soc. 95, 8449 (1973). Absolute stereochemistry: eidem, ibid. 96, 4034 (1974). Biosynthesis: C.-M. Liu et al., J. Antibiot. 30, 416 (1977); 32, 414 (1979). Stereospecific total synthesis: R. E. Dolle, K. C. Nicolaou, J. Am. Chem. Soc. 107, 1691, 1695 (1985). Growth promoting activity: W. L. Marusich et al., Poult. Sci. 53, 636 (1974). Review of chemistry: H. Maehr et al., Can. J. Chem. 58, 501 (1980).

  • Actinobolin CAS Registry Number: 24397-89-5 肌动蛋白


    CAS Name: (2S)-2-Amino-N-[(3R,4R,4aR,5R,6R)-3,4,4a,5,6,7-hexahydro-5,6,8-trihydroxy-3-methyl-1-oxo-1H-2-benzopyran-4-yl]propanamide
    Additional Names: 4-(2-aminopropionamido)-3,4,4a,5,6,7-hexahy...
    Literature References: Antibiotic produced by Streptomyces griseoviridus var atrofaciens; (+)-form is naturally occurring. Isoln and characterization: T. H. Haskell, Q. R. Bartz, Antibiot. Annu. 1958-1959, 505; T. H. Haskell et al., US 3043830 (1962 to Parke, Davis). Structural studies: Struck et al., Tetrahedron Lett. 1967, 1589; Munk et al., J. Am. Chem. Soc. 89, 4158 (1967). Structure: eidem, ibid. 90, 1087 (1968). Absolute configuration and chemistry: Antosz et al., ibid. 92, 4933 (1970). Crystal structure: J. B. Wetherington, J. W. Moncrief, Acta Crystallogr. B31, 501 (1975). Total synthesis: M. Yoshioka et al., J. Am. Chem. Soc. 106, 1133 (1984); eidem, Heterocycles 21, 151 (1984); R. S. Garigipati et al., J. Am. Chem. Soc. 107, 7790 (1985). Antibacterial activity and toxicity: R. F. Pittillo et al., Antibiot. Annu. 1958-1959, 497. Series of articles on antineoplastic activity: ibid. 515-532. Inhibition of protein synthesis: D. Smithers et al., Mol. Pharmacol. 5, 433 (1969). Experimental use as cariostat: D. E. Hunt et al., J. Dent. Res. 50, 371 (1971). Reduction of periodontal syndrome in mice, rats: J. H. Shaw, J. K. Ivimey, Arch. Oral Biol. 18, 357 (1973).

  • Aplasmomycin CAS Registry Number: 61230-25-9 硼酸盐(1-),[(1R,2R,5S,6R,8S,9E,12R,14S,17R,18R,19R,22S,23R,25S,26E,29R,31S,34R)-1,2,18,19-四(羟基-kO)-12,29-二羟基-6,13,13,17,23,30,30,34-辛甲基-4,7,21,24,35,37-六氧喷环[29.3.1.15,8.114,18.122,25]octa三十-9,26-二烯-3,20-dionato(4-)]-,钠(1:1),(T-4)-

    Percent Composition: C 60.15%, H 7.57%, B 1.35%, Na 2.88%, O 28.04%
    Literature References: Antibiotic produced by Streptomyces griseus strain SS-20, obtained from shallow sea mud: Y. Okami et al., J. Antibiot. 29, 1019 (1976); eidem, JP Kokai 77 108901 (1977 to Microbiochem. Res. Found.), C.A. 88, 35843 (1978). It inhibits the growth of gram-positive bacteria in vitro and is active vs Plasmodium berghei in vivo. Aplasmomycin is a symmetrical dimer related to boromycin, q.v., the only other known natural product that contains boron. Structure, x-ray crystallography: H. Nakamura et al., J. Antibiot. 30, 714 (1977). Total synthesis of (+)-form: E. J. Corey et al., J. Am. Chem. Soc. 104, 6816, 6818 (1982); T. Nakata et al., Tetrahedron Lett. 27, 6341, 6345 (1986); J. D. White et al., J. Am. Chem. Soc. 108, 8105 (1986). Use as growth promotant in ruminants: D. H. Davies et al., EP 2893; eidem, US 4225593 (1979, 1980 both to ICI). Two minor components, aplasmomycins B and C, have also been isolated from the fermentation; both aplasmomycin and aplasmomycin B show ionophoric properties, mediating net K+ transport across a bulk phase: K. Sato et al., J. Antibiot. 31, 632 (1978). NMR analysis of aplasmomycin and deboroaplasmomycin: T. S. S. Chen et al., ibid. 33, 1316 (1980). Comparative anti-anaerobic activity of aplasmomycin: K. Watanabe et al., Antimicrob. Agents Chemother. 19, 519 (1981). Structural studies: T. J. Stout et al., Tetrahedron 47, 3511 (1991). Review of biosynthetic studies: H. G. Floss, C. Chang in Antibiotics IV, J. W. Corcoran, Ed. (Springer-Verlag, New York, 1981) pp 203-210.

  • Efrotomycin CAS Registry Number: 56592-32-6 依罗霉素


    CAS Name: 31-O-[6-Deoxy-4-O-(6-deoxy-2,4-di-O-methyl-a-L-mannopyranosyl)-3-O-methyl-b-D-allopyranosyl]-1-methylmocimycin
    Additional Names: 31-O-[6-deoxy-4-O-(6-deoxy-2,4-di-O-methylhexopyranosy...
    Literature References: Antibiotic produced by Streptomyces lactamdurans NRRL 3802: R. G. Wax, W. M. Maiese, DE 2450813 (1975 to Merck Co.), C.A. 83, 145755y (1975); R. G. Wax et al., J. Antibiot. 29, 670 (1976). In vitro and in vivo activity: B. M. Frost et al., ibid. 1083; 32, 626 (1979). Production and growth promoting activity: W. M. Maiese, R. G. Wax, US 4024251 (1977 to Merck Co.). Synergism with bottromycin, q.v.: B. M. Frost et al., J. Antibiot. 32, 1046 (1979). Structure: R. S. Dewey et al., ibid. 38, 1691 (1985). Stereospecific total synthesis: R. E. Dolle, K. C. Nicolaou, J. Am. Chem. Soc. 107, 1691, 1695 (1985). HPLC determn in feeds: J. D. Strong, Analyst 111, 853 (1986). Effect on gain and feed efficiency in swine: A. G. Foster et al., J. Anim. Sci. 65, 877 (1987).

  • Lincomycin CAS Registry Number: 154-21-2 林可霉素


    CAS Name: (2S-trans)-Methyl 6,8-dideoxy-6-[[(1-methyl-4-propyl-2-pyrrolidinyl)carbonyl]amino]-1-thio-D-erythro-a-D-galacto-octopyranoside
    Additional Names: lincolnensinPercent Composition: C 53...
    Literature References: Antibiotic produced by Streptomyces lincolnensis var. lincolnensis. Isoln: D. J. Mason et al., Antimicrob. Agents Chemother. 1962, 555; R. R. Herr, M. E. Bergy, ibid. 560; M. E. Bergy et al., US 3086912 (1963 to Upjohn). Structure: Hoeksema et al., J. Am. Chem. Soc. 86, 4223 (1964). Synthesis: Magerlein, Tetrahedron Lett. 1970, 33. Stereoselective synthesis: S. Knapp, P. J. Kukkola, J. Org. Chem. 55, 1632 (1990). Mechanism of action: F. N. Chang in Antibiotics vol. 5(pt. 1), F. E. Hahn, Ed. (Springer-Verlag, New York, 1979) pp 127-134. Clinical study: F. Puleo et al., Gazz. Med. Ital. 138, 401 (1979). Toxicity data: Gray et al., Toxicol. Appl. Pharmacol. 6, 476 (1964). Comprehensive description: H. Y. Muti, F. H. Al-Hajjar, Anal. Profiles Drug Subs. Excip. 23, 269-319 (1994).

  • Mocimycin CAS Registry Number: 50935-71-2 莫西霉素


    Additional Names: Antibiotic MYC 8003; delvomycin; kirromycinPercent Composition: C 64.81%, H 7.59%, N 3.52%, O 24.09%
    Literature References: Antibiotic produced by Streptomyces ramocissimus. Isoln and properties: C. Vos, J. Den Admirant, DE 2140674; eidem, US 3927211; US 3923981 (1972, 1975, 1975 all to Gist-Brocades). Structural studies: C. Vos, P. E. J. Verwiel, Tetrahedron Lett. 1973, 2823, 5173. Total structure and identity with kirromycin: H. Maehr et al., J. Am. Chem. Soc. 95, 8449 (1973). Absolute stereochemistry: eidem, ibid. 96, 4034 (1974). Conversion to aurodox: H. Maehr et al., J. Antibiot. 32, 361 (1979). Biological studies: H. Wolf et al., Proc. Natl. Acad. Sci. USA 71, 4910 (1974); J. A. M. Van De Klundeit et al., FEBS Lett. 81, 303 (1977). Review of chemistry: H. Maehr et al., Can. J. Chem. 58, 501-526 (1980). Review of properties and actions: A. Parmeggiani, G. Sander, Topics in Antibiotic Chemistry vol. 5, P. G. Sammes, Ed. (Halsted Press, New York, 1980) pp 159-221.

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