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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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Interleukin-2 CAS Registry Number: 85898-30-2 白介素2(人类克隆pTIL2-21a蛋白基团还原)

Additional Names: T-Cell growth factor; TCGF; thymocyte stimulating factor; costimulator; lymphocyte mitogenic factor; IL-2
Literature References: Pleiotropic cytokine produced by T-lymphocytes following activation by antigens or mitogens in the presence of IL-1, q.v. Native, human IL-2 is a glycoprotein containing 133 amino acid residues; mol wt ~15 kDa. Potent immunomodulator with important role in activating and maintaining the immune response. Induces growth and proliferation of CD4+ and CD8+ T cells; enhances natural killer cell activity; stimulates antigen secretion; potentiates the release of g-interferon and other cytokines. Also serves to down-regulate the immune system to prevent autoimmunity. Identification of soluble mitogenic factor produced by T-cells in response to antigen: R. S. Geha, E. Merler, Cell. Immunol. 10, 86 (1974). Identification of T-cell growth promoting factor produced by mitogen stimulated lymphocytes: D. A. Morgan et al., Science 193, 1007 (1976). Definition and nomenclature: L. A. Aarden et al., J. Immunol. 123, 2928 (1979). Induction of IL-2 production by IL-1: K. A. Smith et al., J. Exp. Med. 151, 1551 (1980). Review of early studies: J. Watson, D. Mochizuki, Immunol. Rev. 51, 257 (1980). Purification and partial amino acid sequence: R. J. Robb et al., Proc. Natl. Acad. Sci. USA 80, 5990 (1983). Expression of cloned cDNA for human IL-2 and predicted amino acid sequence: T. Taniguchi et al., Nature 302, 305 (1983). Isolation of human IL-2 gene: S. Mita et al., Biochem. Biophys. Res. Commun. 117, 114 (1983). Purification and cloning of the T-cell surface receptor for IL-2: W. J. Leonard et al., Nature 311, 626 (1984). Review of recombinant IL-2 muteins: L. T. Vlasveld, E. M. Rankin, Cancer Treat. Rev. 20, 275-311 (1994). Review of pharmacology and therapeutic use in cancer: R. Whittington, D. Faulds, Drugs 46, 446-514 (1993); of function, production and clinical applications: S. L. Gaffen, K. D. Liu, Cytokine 28, 109-123 (2004).

Tutin CAS Registry Number: 2571-22-4 羟基马桑毒内酯

CAS Name: (1aS,1bS,2S,2'R,5R,6S,6aR,7aR,8S)-Hexahydro-1b,6-dihydroxy-6a-methyl-8-(1-methylethenyl)spiro[2,5-methano-7H-oxireno[3,4]cyclopent[1,2-d]oxepin-7,2'-oxiran]-3(2H)-one
Percent Composit...
Literature References: Poisonous constituent of Coriaria ruscifolia L. or C. japonica A. Gray, (tutu) Coriariaceae. Naturally occurring form is (+)-tutin. Isoln: Easterfield, Aston, J. Chem. Soc. 79, 125 (1901). Structure: Johns, Markham, ibid. 1961, 3006; Craven, Nature 197, 1193 (1963); Mackay, Mathieson, Tetrahedron Lett. 1963, 1399. Absolute configuration: Okuda, Yoshida, ibid. 1965, 2137. Biosynthesis: A. Corbella et al., Chem. Commun. 1969, 634. NMR analysis: J. W. Blunt et al., Aust. J. Chem. 32, 1339 (1979). Stereospecific synthesis: K. Watamatsu et al., Tetrahedron 42, 5551 (1986). Determn in toxic honey: J. L. Love et al., N.Z. J. Technol. 2, 179 (1986). Effect on central nervous system: D. R. Curtis et al., Brain Res. 63, 419 (1973); A. Nistri et al., Lancet 1, 996 (1974). Toxicity data: C. H. Jarboe et al., J. Med. Chem. 11, 729 (1968).

Alborixin CAS Registry Number: 57760-36-8 白璃霉素

Additional Names: Antibiotic S 14750A
Percent Composition: C 65.13%, H 9.57%, O 25.30%
Literature References: Polycyclic polyether antibiotic ionophore, isolated from a strain of Streptomyces albus. Initial description and x-ray structure: M. Allèaume et al., Chem. Commun. 1975, 411. Production from Streptomyces hygroscopicus and use: M. Kuhn, H. D. King, DE 2608337 (1976 to Sandoz), C.A. 86, 28491k (1977). Isoln from S. albus, structure, properties: P. Gachon et al., J. Antibiot. 29, 603 (1976); C. Delhomme et al., ibid. 692. NMR spectrum and solution conformation: N. A. Rodios, M. J. O. Anteunis, Bull. Soc. Chim. Belg. 88, 279 (1979). Revised structure: H. Seto et al., J. Antibiot. 32, 970 (1979). In vitro study: M. Chapel et al., ibid. 740. Effects on cardiovascular function and plasma cation concentration in the dog: N. Moins et al., J. Cardiovasc. Pharmacol. 1, 659 (1979).

Hamycin CAS Registry Number: 1403-71-0

Additional Names: Primamycin
Literature References: Polyene antibiotic complex produced by Streptomyces pimprina: M. J. Thirumalachar et al., Hind. Antibiot. Bull. 3, 136 (1961), C.A. 55, 27515i (1961); M. J. Thirumalachar, US 3261751 (1966 to Hindustan Antibiot.). Formerly believed to be identical to trichomycin and candicidin, q.q.v.: H. Burrows, D. Calam, J. Chromatogr. 53, 566 (1970). Subsequent HPLC studies have shown the three polyene antibiotics to be different entities: P. Helboe et al., ibid. 189, 249 (1980). Structural study showing hamycin to be a mixture of components A, B, C, D: R. C. Pandey, K. L. Rinehart, 16th Interscience Conference on Antimicrob. Ag. Chemother., Chicago, 1976, Abstracts of Papers, no. 41. Absorption, excretion, tissue concentration: M. G. Phatak et al., Indian J. Exp. Biol. 12, 284 (1974), C.A. 82, 118703j (1975). Toxicity studies: Williams et al., Antimicrob. Agents Chemother. 1964, 737; antifungal activity: A. C. Parekh, C. V. Dave, Life Sci. 19, 1737 (1976). HPLC study: W. Mechlinski, C. P. Schaffner, J. Antibiot. 33, 591 (1980). Review of clinical use in mycoses: M. J. Thirumalachar, J. Sci. Ind. Res. 31, 542-544 (1972), C.A. 79, 13308 (1973).

Amphotericin B CAS Registry Number: 1397-89-3 两性霉素B

Trademarks: Fungizone (BMS); Fungilin (BMS); Ampho-Moronal (BMS)
Percent Composition: C 61.09%, H 7.96%, N 1.52%, O 29.43%
Literature References: Polyene antibiotic produced by Streptomycetes nodosus M4575 obtained from soil of the Orinoco river region of Venezuela: Gold et al., Antibiot. Annu. 1955-1956, 579; Vandeputte et al., ibid. 587; Dutcher et al., ibid. 1956-1957, 866; Walters et al., J. Am. Chem. Soc. 79, 5076 (1957); Dutcher et al., US 2908611 (1959 to Olin Mathieson). Structure studies: Borowski et al., Tetrahedron Lett. 1965, 473. Carbon skeleton, ring size, and partial structure: Cope et al., J. Am. Chem. Soc. 88, 4228 (1966). Complete structure: Mechlinski et al., Tetrahedron Lett. 1970, 3873; Borowski et al., ibid. 3909; R. C. Pandey, K. L. Rinehart, J. Antibiot. 29, 1035 (1976). Total synthesis: K. C. Nicolaou et al., J. Am. Chem. Soc. 109, 2821 (1987). Toxicity: G. R. Keim et al., Science 179, 584 (1973). Comprehensive description: I. M. Asher et al., Anal. Profiles Drug Subs. 6, 1-42 (1977). Review of clinical experience: H. A. Gallis et al., Rev. Infect. Dis. 12, 308-329 (1990); of lipid formulations: J. W. Hiemenz, T. J. Walsh, Clin. Infect. Dis. 22, Suppl. 2, S133-S144 (1996). Review: K. M. Abu-Salah, Br. J. Biomed. Sci. 53, 122-133 (1996).

Nystatin CAS Registry Number: 1400-61-9 制霉菌素

Additional Names: Fungicidin
Trademarks: Biofanal (Pfleger); Diastatin; Candex (Miles); Candio-Hermal (Hermal); Mycostatin (BMS); Moronal (BMS); Nystan (BMS); O-V Statin (BMS)
Literature References: Polyene antifungal antibiotic complex containing 3 biologically active components, A1, A2, A3. Produced by Streptomyces noursei, S. aureus and other Streptomyces spp: Hazen, Brown, Science 112, 423 (1950); Proc. Soc. Exp. Biol. Med. 76, 93 (1951); Raubitscheck et al., Antibiot. Chemother. 2, 179 (1952); Cohen, Webb, Arch. Pediatr. 69, 414 (1952); Dutcher et al., Antibiot. Annu. 1953-1954, 191; eidem, Therapy of Fungus Diseases (Little, Brown, Boston, 1955) p 168. Review of early literature: Brown, Hazen, Trans. N.Y. Acad. Sci. 19 (1956-1957) pp 447-456. Purification: Vandeputte, US 2832719 (1958 to Olin Mathieson); Renella, US 3517100 (1970 to Am. Cyanamid). Chemistry and partial structure: Birch et al., Tetrahedron Lett. 1964, 1491; of nystatin A1 and A2: Shenin et al., Antibiotiki 13, 387 (1968). Structure of the aglycone: Manwaring et al., ibid. 1969, 5319. Complete structure of A1: Chong, Rickards, ibid. 1970, 5145; Borowski et al., ibid. 1971, 685. Revised structure: R. C. Pandey, K. L. Rinehart, J. Antibiot. 29, 1035 (1976). Stereochemical study of A1: J. M. Lancelin et al., Tetrahedron Lett. 29, 2827 (1988). Structure of A3: J. Zielinski et al., J. Antibiot. 41, 1289 (1988). Mechanism of action: R. W. Holz in Antibiotics vol. 5, pt. 2, F. E. Hahn, Ed. (Springer-Verlag, New York, 1979) pp 313-340. Toxicity study: H. Seneca, Antibiot. Annu. 1955-1956, 697. Comprehensive description: G. W. Michel, Anal. Profiles Drug Subs. 6, 341-421 (1977).

Lucensomycin CAS Registry Number: 13058-67-8

Additional Names: Antibiotic FI 1163Trademarks: Etruscomicina; Etruscomycin
Percent Composition: C 61.09%, H 7.55%, N 1.98%, O 29.39%
Literature References: Polyene antifungal antibiotic isolated from cultures of Streptomyces lucensis: Arcamone et al., G. Microbiol. 4, 119 (1957); Arcamone, Perego, Ann. Chim. (Rome) 49, 345 (1959); Marini, Pennella, Proc. Symp. Antibiotics Prague (May 1959) p 148; Arcamone et al., US 3170837 (1965 to Farmitalia). Structure: Guadiano et al., Tetrahedron Lett. 1966, 3559, 3567; Gazz. Chim. Ital. 96, 1470 (1966); Chim. Ind. (Milan) 48, 1327 (1966). Revised structure: R. C. Pandey, K. L. Rinehart, J. Antibiot. 29, 1035 (1976).

Natamycin CAS Registry Number: 7681-93-8 纳他霉素

CAS Name: Pimaricin
Additional Names: antibiotic A 5283; tennecetinTrademarks: Mycophyt (Mycofarm); Myprozine (Am. Cyanamid); Natacyn (Alcon); Pimafucin (Basotherm); Synogil (Basotherm)
Perc...
Literature References: Polyene antifungal antibiotic produced by Streptomyces natalensis from soil near Pietermaritzburg, South Africa and by S. chattanoogensis. Isoln: Struyk et al., Antibiot. Annu. 1957-1958, 878. Prodn: GB 844289 (1960 to Koninklijke Nederlandsche Gist en Spiritus-Fabriek); GB 846933 (1960 to Am. Cyanamid). Identity with tennecetin: Divekar et al., Antibiot. Chemother. 11, 377 (1961). Structure: Golding et al., Tetrahedron Lett. 1966, 3551; Meyer, Chem. Commun. 1968, 470. Configuration: Gaudiano et al., Chim. Ind. (Milan) 48, 1327 (1966). Revised structure: R. C. Pandey, K. L. Rinehart, J. Antibiot. 29, 1035 (1976). Soly data: Marsh, Weiss, J. Assoc. Off. Anal. Chem. 50, 457 (1967). Toxicology: G. J. Levinskas et al., Toxicol. Appl. Pharmacol. 8, 97 (1966). Comprehensive description: H. Brik, Anal. Profiles Drug Subs. Excip. 23, 399-419 (1994).

Phytofluene CAS Registry Number: 540-05-6 (6E,10E,12E,14E,16E,18E,22E,26E)-2,6,10,14,19,23,27,31-八甲基三十二碳-2,6,10,12,14,16,18,22,26,30-十烯

CAS Name: 7,7',8,8',11,12-Hexahydro-y,y-carotene
Additional Names: 5,6,7,8,9,10,10',9',8',7',6',5'-dodecahydrolycopene; all-trans-phytofluene
Percent Composition: C 87.51%, H 12.49%
Literature References: Polyene hydrocarbon widespread in the vegetable kingdom where it has been observed in chlorophyll-free tissues which contain considerable amounts of carotenoid pigments. Extracted from Diospyros kaki L.f., Ebenaceae, Arbutus unedo L., Ericaceae, Pyracantha angustifolia (Franch.) Schneid., Rosaceae, and tomatoes: Zechmeister, Sandonal, J. Am. Chem. Soc. 68, 197 (1946); Wallace, Porter, Arch. Biochem. Biophys. 36, 468 (1952); from the basidiomycete, Dacromyces stillatus: Goodwin, Biochem. J. 53, 538 (1953). Structure: Porter, Lincoln, Arch. Biochem. Biophys. 27, 390 (1950); Zechmeister, Experientia 10, 1 (1954).

Maduramicin CAS Registry Number: 84878-61-5 马度米星

CAS Name: (2R,3S,4S,5R,6S)-6-[(1R)-1-[(2S,5R,7S,8R,9S)-2-[(2S,2'R,3'S,5R,5'R)-3'-[(2,6-Dideoxy-3,4-di-O-methyl-b-L-arabino-hexopyranosyl)oxy]octahydro-2-methyl-5'-[(2S,3S,5R,6S)-tetrahydro-6-hydro...
Literature References: Polyether antibiotic chemically related to the lonomycins, q.v. Isoln as sodium salt from Nocardia sp X-14868 and biological activity: C.-M. Liu et al., US 4278663 (1981 to Hoffmann-La Roche); as free acid hydrate from Actinomadura yumaense sp nov.: D. P. Labeda et al., US 4407946 (1983 to Am. Cyanamid). Fermentation and properties: C.-M. Liu et al., J. Antibiot. 36, 343 (1983). 13C-NMR spectrum: S. Rajan, ibid. 37, 1495 (1984). Biosynthetic studies: H.-R. Tsou et al., ibid. 1651; H.-R. Tsou et al., ibid. 40, 94 (1987). Antimalarial activity: L. Oronsky, US 4496549 (1985 to Am. Cyanamid). Nematocidal activity: I. B. Wood, US 4510134 (1985 to Am. Cyanamid).