其它产品项目整合

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

Encainide CAS Registry Number: 66778-36-7 (±)-4-甲氧基-N-[2-[2-(1-甲基-2-哌啶基)乙基]苯基]苯甲酰胺

CAS Name: 4-Methoxy-N-[2-[2-(1-methyl-2-piperidinyl)ethyl]phenyl]benzamide
Additional Names: (±)-2'-[2-(1-methyl-2-piperidyl)ethyl]-p-anisanilide; 4-methoxy-2'-[2-(1-methyl-2-piperidyl)eth...
Literature References: Anti-arrhythmic benzanilide derivative. Prepn: S. J. Dykstra, J. L. Minielli, DE 2210154 (1972 to Bristol-Myers), C.A. 78, 4138j (1973); eidem, US 3931195 (1976 to Mead Johnson); S. J. Dykstra et al., J. Med. Chem. 16, 1015 (1973). Anti-arrhythmic pharmacology in animals: J. E. Byrne et al., J. Pharmacol. Exp. Ther. 200, 147 (1977). Clinical pharmacology and efficacy in chronic ventricular arrhythmia: D. M. Roden et al., N. Engl. J. Med. 302, 877 (1980). Electrophysiology and effects on cardiac conduction: M. Sami et al., Am. J. Cardiol. 44, 526 (1979). Hemodynamic effects: M. Sami et al., ibid. 52, 507 (1983). Adverse effects: R. A. Winkle et al., Am. Heart J. 102, 857 (1981). Comparison with other Class I anti-arrhythmic agents: A. Pottage, Am. J. Cardiol. 52, 24C (1983). Series of articles on pharmacology, pharmacokinetics, metabolism, clinical safety and efficacy: ibid. 58(5), 1C-116C (1986). Review: L. B. Mitchell, R. A. Winkle in New Drugs Annual: Cardiovascular Drugs vol. 1, A. Scriabine, Ed. (Raven Press, New York, 1983) pp 93-107.

Clinofibrate CAS Registry Number: 30299-08-2 克利贝特

CAS Name: 2,2'-[Cyclohexylidenebis(4,1-phenyleneoxy)]bis[2-methylbutanoic acid]
Additional Names: 2,2'-(4,4'-cyclohexylidenediphenoxy)-2,2'-dimethyldibutyric acidTrademarks: Lipoclin (Sumitomo)...
Literature References: Anti-atherosclerosis agent, related structurally to clofibrate, q.v. Prepn: Y. Nakamura et al., DE 2017331; eidem, US 3716583 (1970, 1973 both to Sumitomo). Hypolipidemic activity: K. Toki et al., Atherosclerosis 18, 101 (1973); K. Suzuki et al., Jpn. J. Pharmacol. 24, 407 (1974), C.A. 82, 25821z (1975). Effect on cholesterol and lipoprotein metabolism in rats: K. Suzuki, Biochem. Pharmacol. 25, 325 (1976). General pharmacology: H. Nakatani et al., Oyo Yakuri 16, 687 (1978), C.A. 90, 145808 (1979).

Fuscin CAS Registry Number: 83-85-2 暗褐菌素

CAS Name: 9,10-Dihydro-5-hydroxy-4,8,8-trimethyl-2H,4H-benzo[1,2-b:4,3-c']dipyran-2,6(8H)-dione
Percent Composition: C 65.21%, H 5.84%, O 28.96%
Literature References: Antibacterial pigment produced by the fungus Oidiodendron fuscom Robak: Michael, Biochem. J. 42, XL; 43, 528 (1948). Derivatives and degradation products: Birkinshaw et al., ibid. 48, 66 (1951). Structure and synthesis: Birch, Chem. Ind. (London) 1955, 682; Barton, Hendrickson, J. Chem. Soc. 1956, 1028. Alternate synthesis: Pyuskyulev et al., Tetrahedron 29, 2849 (1973). Biosynthesis: Birch, Ciba Found. Symp. Quinones Electron Transp. 1960, 233; Birch et al., J. Chem. Soc. 1965, 1231.

Fusaric Acid CAS Registry Number: 536-69-6 5-丁基吡啶-2-羧酸

CAS Name: 5-Butyl-2-pyridinecarboxylic acid
Additional Names: 5-butylpicolinic acid
Percent Composition: C 67.02%, H 7.31%, N 7.82%, O 17.85%
Literature References: Antibiotic (wilting agent) first isolated from the fungus Fusarium heterosporium, Nees: Yabuta et al., J. Agric. Chem. Soc. Jpn. 10, 1059 (1934). Isoln from other Fusarium species and from Gibberella fujikuroi and synthesis: Plattner et al., Helv. Chim. Acta 37, 1379 (1954). Prepn: Hardegger, Nikles, ibid. 39, 505 (1956); 40, 2428 (1957); Schreiber, Adam, Ber. 93, 1848 (1960); Umezawa, Nagatsu, DE 2005255 (1970 to Microbiochem. Res. Found.); R. Tschesche, W. Führer, Ber. 111, 3502 (1978). Dopamine b-hydroxylase inhibitor and hypotensive activity: Suda et al., Chem. Pharm. Bull. 17, 2377 (1969); Nagatsu et al., Biochem. Pharmacol. 19, 35 (1970). Toxicity study: Ishii et al., Arzneim.-Forsch. 25, 55 (1975).

Sarkomycin CAS Registry Number: 11031-48-4

Additional Names: Sarcomycin
Literature References: Antibiotic and antitumor substance produced by Streptomyces erythrochromogenes, strain W-115-C, from soil found at Kamakura, Japan: Umezawa et al., J. Antibiot. 6A, 101, 147, 153 (1953); eidem, Antibiot. Chemother. 4, 514 (1954). Structure of sarkomycin A, the active principle: Hooper et al., ibid. 5, 585 (1955). Characterization of sarkomycins A, A¢ and B: Maeda, Kondo, J. Antibiot. 11A, 37 (1958). Sarkomycin reacts with H2S to form sarkomycins S1, S2 and S3: Tatsuoka et al., ibid. 9B, 107, 110 (1956). Structure of S1 and S2: eidem, ibid. 11B, 275 (1958). Synthesis of d- and l-sarkomycin A: Toki, ibid. 10A, 35, 226 (1957). Synthesis of dl-sarkomycin A: Toki, Bull. Chem. Soc. Jpn. 30, 450 (1957); R. K. Boeckman, Jr. et al., J. Org. Chem. 45, 752 (1980); J. N. Marx, G. Minaskanian, ibid. 47, 3306 (1982); B. A. Wexler et al., ibid. 3333; A. P. Kozikowski, P. D. Stein, J. Am. Chem. Soc. 104, 4023 (1982). Abs config of A: Sato et al., Chem. Pharm. Bull. 11, 829 (1963). Revised config of A: Hill et al., J. Org. Chem. 32, 2330 (1967). Review: S. A. Waksman, H. A. Lechevalier, The Actinomycetes vol. III (Williams Wilkins, Baltimore, 1962) pp 362-364; Sung in Antibiotics vol. I, D. Gottlieb, P. Shaw, Eds. (Springer-Verlag, New York, 1967) pp 156-165.

Aureothin CAS Registry Number: 2825-00-5 金链菌素

CAS Name: (Z,E)-2-Methoxy-3,5-dimethyl-6-[tetrahydro-4-[2-methyl-3-(4-nitrophenyl)-2-propenylidene]-2-furanyl]-4H-pyran-4-one
Additional Names: mycolutein
Percent Composition: C 66.49%, H 5....
Literature References: Antibiotic by-product of aureothricin, q.v., isolated from the culture of Streptomyces thioluteus. Isoln: K. Maeda, J. Antibiot. 6A, 137 (1953); (as mycolutein): H. Schmitz, R. Woodside, Antibiot. Chemother. 5, 652 (1955). Structure: Y. Hirata et al., Tetrahedron 14, 252 (1961). Identity with mycolutein: J. L. Schwartz et al., J. Antibiot. 29, 236 (1976). Biosynthesis: R. Cardillo et al., Tetrahedron 30, 459 (1974); M. Yamazaki et al., Chem. Pharm. Bull. 23, 569 (1975). Synthesis: Y. Shizuri et al., Chem. Lett. 1987, 1381.

Gentamicin CAS Registry Number: 1403-66-3 庆大霉素C1a

CAS Name: Gentamycin
Literature References: Antibiotic complex produced by fermentation of Micromonospora purpurea or M. echinospora and variants thereof: M. J. Weinstein et al., Antimicrob. Agents Chemother. 1963, 1. Isoln, purification and characterization: J. P. Rosselet et al., ibid. 14. Industrial pats.: G. M. Luedemann, M. J. Weinstein; Charney, US 3091572; US 3136704 (1963, 1964, both to Schering). Consists of three closely related components, gentamicins C1, C2, C1a, and also gentamicin A which differs from the other members of the complex but is similar to kanamycin C, q.v. Separation of gentamicin C components: H. Maehr, C. P. Schaffner, J. Chromatogr. 30, 572 (1967); Wagman et al., ibid. 34, 210 (1968). Structures contain 2-deoxystreptamine, q.v., linked to two saccharide units, these being garosamine and a purpurosamine in the C series gentamicins. Structure studies: D. J. Cooper et al., J. Chem. Soc. C 1971, 960, 2876, 3126. Structure of gentamicin A: H. Maehr, C. P. Schaffner, J. Am. Chem. Soc. 89, 6787 (1967); 92 1697 (1969). Sepn and structures of gentamicins A1 to A4: Nagabhushan et al., J. Org. Chem. 40, 2830, 2835 (1975). Synthetic studies: W. Meyer zu Reckendorf, Bischof, Ber. 105, 2546 (1972); M. Chmielewski et al., Carbohydr. Res. 70, 275 (1979). Review of activity, toxicity and clinical pharmacology: J. Black et al., Antimicrob. Agents Chemother. 1963, 138-147. Comprehensive description: B. E. Rosenkrantz et al., Anal. Profiles Drug Subs. 9, 295-340 (1980). Determn in serum by immunoassay: H. A. Holt et al., J. Antimicrob. Chemother. 34, 747 (1994). Review of clinical use: S. B. Shrimpton et al., ibid. 31, 599-606 (1993). Clinical effect on chloride transport in cystic fibrosis: M. Wilschanski et al., Am. J. Respir. Crit. Care Med. 161, 860 (2000).

Xanthocillin CAS Registry Number: 11042-38-9

Additional Names: Xantocillin
Trademarks: Brevicid (AWD)
Literature References: Antibiotic complex produced by Penicillium notatum Westling: Rothe, Pharmazie 5, 190 (1950); Barwald, GB 898498 (1962 to Arzneimittelwerk VEB), C.A. 57, 9013a (1962). Consists of at least three antibiotics, xanthocillins X, Y1 and Y2; the first being the major component (about 70%).

Cactinomycin CAS Registry Number: 8052-16-2 放线菌素C

CAS Name: Actinomycin CTrademarks: Sanamycin (FBA Pharm)
Literature References: Antibiotic complex produced by Streptomyces chrysomallus: Brockmann, Grubhofer, Naturwissenschaften 36, 376 (1949); 37, 494 (1950); Ber. 84, 260 (1951); US 2953495 (1960 to Shenley Inds.); Lindenbein, Arch. Mikrobiol. 17, 361 (1952). Mixture of actinomycins C1 (dactinomycin, q.v.), C2 and C3, 10%, 45% and 45%, resp: Brockmann, Pfennig, Naturwissenschaften 39, 429 (1952); Brockmann, Gröne, ibid. 40, 222 (1953). Description of other actinomycins: Waksman et al., Proc. Natl. Acad. Sci. USA 44, 602 (1958). Structures: Brockmann et al., Angew. Chem. 68, 70 (1956); Brockmann, Boldt, Naturwissenschaften 50, 19 (1963). Synthesis of actinomycin C3: Brockmann, Lackner, ibid. 47, 230 (1960); 48, 555 (1961); 51, 407 (1964); Brockmann et al., DE 1172680 (1964 to Bayer); Brockmann, Lackner, Ber. 100, 353 (1967); 101, 1312 (1968). Synthesis of actinomycin C2: Brockmann, Lackner, Tetrahedron Lett. 1964, 3517. Comprehensive review: H. Brockmann, in Fortschr. Chem. Org. Naturst. 18, 1-54 (1960).

Leptomycin B CAS Registry Number: 87081-35-4 来普霉素B

CAS Name: (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-19-[(2S,3S)-3,6-Dihydro-3-methyl-6-oxo-2H-pyran-2-yl]-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo-2,10,12,16,18-nonadecapentaenoic acid
Addi...
Literature References: Antibiotic compound with antifungal and antitumor activity. Inhibits the CRM1/exportin1 pathway of nuclear transport in eukaryotic cells, facilitating its use in the study of nuclear export. Isoln from Streptomyces sp. ATS1287: T. Hamamoto et al., J. Antibiot. 36, 639 (1983); from actinomycete ATCC 39366: G. C. Hokanson et al., EP 139458; eidem, US 4771070 (1985, 1988 both to Warner Lambert). Antitumor activity: B. J. Roberts et al., Cancer Chemother. Pharmacol. 16, 95 (1986); and antimicrobial activity: J. B. Tunac et al., J. Antibiot. 38, 460 (1985). Synthesis and abs config: M. Kobayashi et al., Tetrahedron Lett. 39, 8291 (1998). HPLC determn in fermentation extracts: M. Stadler et al., J. Chromatogr. A 818, 187 (1998). Review of use as inhibitor of nuclear export: M. Yoshida et al., Actinomycetologica 12, 120-128 (1998).