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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

  • Eledoisin CAS Registry Number: 69-25-0 依来多新


    Percent Composition: C 54.58%, H 7.21%, N 15.32%, O 20.19%, S 2.70%
    Literature References: A hendecapeptide from the posterior salivary glands of eledone spp (small octopus spp): Anastasi, Erspamer, Br. J. Pharmacol. 19, 326 (1962); eidem, Experientia 18, 58 (1962). Synthesis: Sandrin, Boissonnas, ibid. 59; eidem, Helv. Chim. Acta 47, 1294 (1964); Lubke et al., Ann. 679, 195 (1964); GB 984810 (1965 to Farmitalia); solid-phase synthesis: P. G. Pietta et al., J. Org. Chem. 39, 44 (1974). Its physiologic action resembles that of the other tachykinins, substance P and physalaemin, q.q.v. Stimulates extravascular smooth muscle, acts as a potent vasodilator and hypotensive agent; in certain species causes salivation, and increases capillary permeability. Pharmacology: Erspamer, Erspamer, Br. J. Pharmacol. 19, 337 (1962); Sicuteri et al., Experientia 19, 44 (1963); G. Bertaccini, Pharmacol. Rev. 28, 127 (1976). Review: Erdös, Adv. Pharmacol. 4, 64-72 (1966).

  • Polytetrafluoroethylene CAS Registry Number: 9002-84-0 聚四氟乙烯


    CAS Name: Tetrafluoroethene homopolymer
    Additional Names: tetrafluoroethylene polymer; polytetrafluoroethylene resin; polytef; PTFE
    Trademarks: Fluon (ICI); Teflon (DuPont); Tetran (Elf Atoc...
    Literature References: A highly stable thermoplastic tetrafluoroethylene, q.v., homopolymer. Composed of at least 20,000 C2F4 monomer units linked into very long unbranched chains. Prepd by polymerization of tetrafluoroethylene: Plunkett, US 2230654 (1941 to Kinetic Chem.); Brubaker, US 2393967; Joyce, US 2394243 (both 1946 to du Pont); Hanford, Joyce, J. Am. Chem. Soc. 68, 2082 (1946); Renfrew, US 2534058 (1950 to du Pont); C. E. Schildknecht, Vinyl and Related Polymers (Wiley, New York, 1952) pp 483-494. Account of discovery by Roy J. Plunkett: A. B. Garrett, J. Chem. Educ. 39, 288 (1962). Reviews: M. M. Renfrew, E. E. Lewis, Ind. Eng. Chem. 38, 870-877 (1946); R. W. Moncrieff, Man-Made Fibres (John Wiley, New York, 4th ed., 1963) pp 512-517; McCane in Encyclopedia of Polymer Science and Technology vol. 13, N. M. Bikales, Ed. (Interscience, New York, 1970) pp 623-654; S. V. Gangal in Kirk-Othmer Encyclopedia of Chemical Technology vol. 11 (Wiley-Interscience, New York, 4th ed., 1994) pp 621-644.

  • Kallidin CAS Registry Number: 342-10-9


    CAS Name: N2-L-Lysylbradykinin
    Additional Names: kallidin-10; kallidin II
    Percent Composition: C 56.60%, H 7.21%, N 20.04%, O 16.16%
    Literature References: A hypotensive and smooth muscle-stimulating principle formed by the proteolysis of kininogen by glandular and other kallikreins, q.v. The decapeptide structure is a homologue of bradykinin, q.v.: Werle et al., Z. Physiol. Chem. 326, 174 (1961). Synthesis: Nicolaides et al., Biochem. Biophys. Res. Commun. 6, 210 (1961); Pless et al., Helv. Chim. Acta 45, 394 (1962).

  • TRH CAS Registry Number: 24305-27-9 普罗瑞林


    CAS Name: 5-Oxo-L-prolyl-L-histidyl-L-prolinamide
    Additional Names: thyrotropin-releasing factor; thyrotropin releasing hormone; TRF; protirelin; lopremone (rescinded USAN); TSH-releasing facto...
    Literature References: A hypothalamic neurohormone which stimulates the release and synthesis of TSH, q.v., from the anterior pituitary via the hypophyseal portal system; the first of the hypothalamic regulatory hormones to be isolated, characterized, and synthesized. Isoln from bovine hypothalami: Schreiber et al., Experientia 18, 338 (1962); Schally et al., Endocrinology 78, 726 (1966). Purification from ovine hypothalami: Guillemin et al., C.R. Seances Acad. Sci. Ser. D 262, 2278 (1966). Isoln from porcine hypothalami and properties: Schally et al., Biochem. Biophys. Res. Commun. 25, 165 (1966); Schally et al., J. Biol. Chem. 244, 4077 (1969). Structural studies: Folkers et al., Biochem. Biophys. Res. Commun. 37, 123 (1969); Burgus et al., C.R. Seances Acad. Sci. Ser. D 269, 226 (1969). Identity of isolated TRH with synthetic tripeptide: Burgus et al., ibid. 1870; Bowers et al., Endocrinology 86, 573, 1143 (1970). Solubility: Burgus et al., Experientia 23, 417 (1967). Synthesis: Flouret, J. Med. Chem. 13, 843 (1970); Chang et al., ibid. 14, 481 (1971); E. Gross et al., Angew. Chem. Int. Ed. 12, 664 (1972); P. G. Pietta et al., J. Org. Chem. 39, 44 (1974). Review of synthetic methods: Rivier, Methods Enzymol. 37, 408 (1975). TRH is also believed to induce the secretion of the pituitary lactogenic hormone, prolactin, q.v.: Tasjian et al., Biochem. Biophys. Res. Commun. 43, 516 (1971); Bowers et al., ibid. 51, 512 (1973). It has been shown to block and reverse leukotriene-induced hypotension in the unanesthetized guinea pig: W. E. Lux et al., Nature 302, 822 (1983). Clinical studies: Hershman, N. Engl. J. Med. 290, 886 (1974). Reviews of TRH and other hypothalamic releasing hormones: Schally et al., Recent Prog. Horm. Res. 24, 497 (1968); Burgus, Guillemin, Annu. Rev. Biochem. 39, 499 (1970); Polypeptide Hormones, R. F. Beers, E. G. Bassett, Eds. (Raven Press, New York, 1980) pp 165-278.

  • Lactobacillic Acid CAS Registry Number: 19625-10-6 (11R,12S)-乳酸杆菌酸


    CAS Name: 2-Hexylcyclopropanedecanoic acid
    Additional Names: 11,12-methyleneoctadecanoic acid; phytomonic acid
    Percent Composition: C 76.97%, H 12.24%, O 10.79%
    Literature References: A lipid constituent of various microorganisms. Isoln from Lactobacillus arabinosus: K. Hofmann, R. A. Lucas, J. Am. Chem. Soc. 72, 4328 (1950); from Agrobacterium tumefaciens and identity of phytomonic acid with lactobacillic acid: K. Hofmann, F. Tausig, J. Biol. Chem. 213, 425 (1955). Structure: K. Hofmann et al., J. Am. Chem. Soc. 80, 5717 (1958). Abs config: J. F. Tocanne, Tetrahedron 28, 363 (1972).

  • Polylysine CAS Registry Number: 25104-18-1 聚赖氨酸


    CAS Name: L-Lysine, homopolymer
    Literature References: A lysine polypeptide or homopolymer, the chain length of which varies with the method of prepn. Prepn: Katchalski et al., J. Am. Chem. Soc. 69, 2564 (1947); 70, 2094 (1948); Fasman et al., ibid. 83, 709 (1961); Sela et al., Biopolymers 1, 517 (1963); Strojny, White, US 3215684 (1965 to Dow). For structure see Lysine.

  • L -Saccharopine CAS Registry Number: 997-68-2 L-酵母氨酸


    CAS Name: N-(5-Amino-5-carboxypentyl)-L-glutamic acid
    Additional Names: e-N-(L-glutar-2-yl)-L-lysine
    Percent Composition: C 47.82%, H 7.30%, N 10.14%, O 34.74%
    Literature References: A lysine precursor in the aminoadipic acid-lysine pathway in yeast: Darling, Larsen, Acta Chem. Scand. 15, 743 (1961); Kjaer, Larsen, ibid. 750; Kuo et al., Biochem. Biophys. Res. Commun. 8, 227 (1962); Trupin, Broquist, J. Biol. Chem. 240, 2524 (1965); Jones, Broquist, ibid. 241, 3430 sqq. (1966). Isoln from mycelium of the yeast Candida utilis: Marimoto, Yamano, Biochem. Z. 340, 155 (1964).

  • Glucose CAS Registry Number: 50-99-7 D(+)-无水葡萄糖


    Additional Names: D-Glucose; dextrose; blood sugar; grape sugar; corn sugar
    Trademarks: Dextropur; Dextrosol; Glucolin
    Percent Composition: C 40.00%, H 6.71%, O 53.28%
    Literature References: A main source of energy for living organisms. Occurs naturally and in the free state in fruits and other parts of plants. Combined in glucosides, in di- and oligosaccharides, in the polysaccharides cellulose and starch, and in glycogen. Normal human blood contains 0.08-0.1%. Manuf on a large scale from starch: Dean, Gottfried, Adv. Carbohydr. Chem. 5, 127 (1950). Below 50°, a-D-glucose hydrate is the stable cryst form, above 50° the anhydr form is obtained and at still higher temps b-D-glucose is formed: W. Pigman, The Carbohydrates (Academic Press, New York, 1957) p 92. Structure: Kjaer, Lindberg, Acta Chem. Scand. 13, 1713 (1959). Conformation: E. Percival, Structural Carbohydrate Chemistry (J. Garnet Miller, London, 1962) pp 51-57. Comprehensive monograph: H. Bartelheimer et al., D-Glucose und verwandte Verbindungen in Medizin und Biologie (Enke, Stuttgart, 1966) 1126 pp.

  • Colchicine CAS Registry Number: 64-86-8 秋水仙碱


    CAS Name: N-[(7S)-5,6,7,9-Tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl]acetamide
    Percent Composition: C 66.15%, H 6.31%, N 3.51%, O 24.03%
    Literature References: A major alkaloid of Colchicum autumnale L., Liliaceae. Extraction procedure: Chemnitius, J. Prakt. Chem. [II] 118, 29 (1928); F. E. Hamerslag, Technology and Chemistry of Alkaloids (New York, 1950) pp 66-80. Structure: Dewar, Nature 155, 141 (1945); King et al., Acta Crystallogr. 5, 437 (1952); Horowitz, Ullyot, J. Am. Chem. Soc. 74, 487 (1952). Crystal structure: L. Lessinger, T. N. Margulis, Acta Crystallogr. B34, 578 (1978). Total synthesis: Schreiber et al., Helv. Chim. Acta 44, 540 (1961); Van Tamelen et al., Tetrahedron 14, 8 (1961); Nakamura, Chem. Pharm. Bull. 8, 843 (1960); Sunagawa et al., ibid. 9, 81 (1961); 10, 281 (1962); Scott et al., Tetrahedron 21, 3605 (1965); Woodward, Harvey Lectures, Ser. 59 (Academic Press, New York, 1965) p 31; Kotani et al., Chem. Commun. 1974, 300; D. A. Evans et al., J. Am. Chem. Soc. 103, 5813 (1981). Biosynthesis: Leete, Tetrahedron Lett. 1965, 333; Battersby et al., J. Chem. Soc. 1964, 4257; Hill, Unrau, Can. J. Chem. 43, 709 (1965). Tubulin-binding activity: J. M. Andreu, S. N. Timasheff, Proc. Natl. Acad. Sci. USA 79, 6753 (1982). Toxicity: S. J. Rosenbloom, F. C. Ferguson, Toxicol. Appl. Pharmacol. 13, 50 (1968); R. P. Beliles, ibid. 23, 537 (1972). Clinical evaluations in cirrhosis of the liver: M. M. Kaplan et al., N. Engl. J. Med. 315, 1448 (1986); D. Kershenobich et al., ibid. 318, 1709 (1988). Bibliography of early literature: Eigsti, Lloydia 10, 65 (1947). Monograph: O. J. Eigsti, P. Dustin, Jr., Colchicine in Agriculture, Medicine, Biology and Chemistry (Iowa State College Press, Ames, Iowa, 1955). Reviews: Fleming, Selected Organic Syntheses (John Wiley, London, 1973) pp 183-207; G. Lagrue et al., Ann. Med. Interne 132, 496-500 (1981); F. D. Malkinson, Arch. Dermatol. 118, 453-457 (1982). Comprehensive description: D. K. Wyatt et al., Anal. Profiles Drug Subs. 10, 139-182 (1981).

  • Chenodiol CAS Registry Number: 474-25-9 鹅去氧胆酸; 鹅脱氧胆酸


    CAS Name: (3a,5b,7a)-3,7-Dihydroxycholan-24-oic acid
    Additional Names: 3a,7a-dihydroxy-5b-cholanic acid; anthropodesoxycholic acid; gallodesoxycholic acid; 17b-(1-methyl-3-carboxypropyl)etiocho...
    Literature References: A major bile acid in many vertebrates, occurring as the N-glycine and/or N-taurine conjugate. With other bile acids, forms mixed micelles with lecithin in bile which solubilize cholesterol and thus facilitates its excretion. Facilitates fat absorption in the small intestine by micellar solubilization of fatty acids and monoglycerides. Has cathartic properties since it induces fluid secretion from large intestine. Main constituent of the bile of hens, geese and other fowl; occurs in appreciable amounts in the bile of hamster, hog, guinea pig, bear and man. Epimeric with ursodiol, q.v. Isoln: Windhaus et al., Z. Physiol. Chem. 140, 177 (1924); Wieland, Reveney, ibid. 186. Configuration: Lettré, Ber. 68, 766 (1935). Prepn from cholic acid: Fieser, Rajagopalan, J. Am. Chem. Soc. 72, 5530 (1950); Hauser et al., Helv. Chim. Acta 43, 1595 (1960); Hofmann, Acta Chem. Scand. 17, 173 (1963). Alternate prepns: Sato, Ikekawa, J. Org. Chem. 24, 1367 (1959); T. Iida, F. C. Chang, ibid. 46, 2786 (1981). Stereoselective total synthesis: T. Kametani et al., J. Am. Chem. Soc. 103, 2890 (1981). Asymmetric total synthesis of (+)-form: eidem, J. Org. Chem. 47, 2331 (1982). Dissolution of cholesterol gallstones: Danzinger et al., N. Engl. J. Med. 286, 1 (1972); Bell et al., Lancet II, 1213 (1972). Use in long-term treatment of cerebrotendinous xanthomatosis: V. M. Berginer et al., N. Engl. J. Med. 311, 1649 (1984). Monograph on bile acids: The Bile Acids, 2 vols., P. P. Nair, D. Kritchevsky, Eds. (Plenum Press, New York, 1971, 1973). Review of pharmacology and therapeutic use of chenodeoxycholic acid: J. H. Iser, A. Sali, Drugs 21, 90-119 (1981). Effect on cholesterol and bile acid metabolism: G. S. Tint et al., Gastroenterology 91, 1007 (1986).

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