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

Arbekacin CAS Registry Number: 51025-85-5 阿贝卡星

CAS Name: O-3-Amino-3-deoxy-a-D-glucopyranosyl-(1®6)-O-[2,6-diamino-2,3,4,6-tetradeoxy-a-D-erythro-hexopyranosyl-(1®4)]-N1-[(2S)-4-amino-2-hydroxy-1-oxobutyl]-2-deoxy-D-streptamine
Additional N...
Literature References: Aminoglycoside antibiotic; derivative of kanamycin B, q.v. Prepn and antibacterial activity: S. Kondo et al., J. Antibiot. 26, 412 (1973); H. Umezawa et al., DE 2350169; eidem, US 4107424 (1974, 1978 both to Microbiochem. Res. Found.). Mechanism of action: N. Tanaka et al., Antimicrob. Agents Chemother. 24, 797 (1983); K. Matsunaga et al., J. Antibiot. 37, 596 (1984). Pharmacology: J. Stewens et al., Arzneim.-Forsch. 35, 1440 (1985); M. Kurebe et al., ibid. 36, 1511 (1986). Series of articles on antibacterial activity, pharmacology, pharmacokinetics, and clinical experience: Chemotherapy 34, Suppl. 1, pp 1-670 (1986). Review: Y. Kobayashi et al., Int. J. Antimicrob. Agents 5, 227-230 (1995).

Isepamicin CAS Registry Number: 58152-03-7 异帕米星

CAS Name: O-6-Amino-6-deoxy-a-D-glucopyranosyl-(1®4)-O-[3-deoxy-4-C-methyl-3-(methylamino)-b-L-arabinopyranosyl-(1®6)]-N1-[(2S)-3-amino-2-hydroxy-1-oxopropyl]-2-deoxy-D-streptamine
Additional N...
Literature References: Aminoglycoside antibiotic; semisynthetic derivative of gentamicin B. Prepn: M. J. Weinstein et al., BE 818431; J. J. Wright, P. J. L. Daniels, BE 824657 (both 1975 to Sherico); J. J. Wright et al., US 4002742 (1977 to Schering Corp.); T. L. Nagabhushan et al., J. Antibiot. 31, 681 (1978). Antibacterial spectrum in vitro and in vivo: G. H. Miller et al., ibid. 688. Comparison with amikacin of nephrotoxic potential: L. I. Rankin et al., Antimicrob. Agents Chemother. 16, 491 (1979). Series of articles on antibacterial activity, toxicology and clinical efficacy: Chemotherapy (Tokyo) 35, Suppl 5, 1-610 (1985); on toxicology: Jpn. J. Antibiot. 39, 3164-3328 (1986), C.A. 107, 32666r-32673r (1987). Acute toxicity: T. Morino et al., ibid. 3164, C.A. 107, 32667s (1987).

Butirosin CAS Registry Number: 12772-35-9 布替罗星

Additional Names: Ambutyrosin
Percent Composition: C 45.40%, H 7.44%, N 12.61%, O 34.56%
Literature References: Aminoglycosidic antibiotic complex obtained from fermentation filtrates of mucoid strains of Bacillus circulans (NRRL B-3312 and B-3313). Consists of two components, butirosin A (80-85%) and butirosin B (15-20%), isomers which differ only in the configuration at one carbon atom in the pentose moiety. Prepn: P. W. K. Woo et al., DE 1914527; eidem, US 3541078 (1969, 1970 both to Parke, Davis). Isoln and characterization: Dion et al., Antimicrob. Agents Chemother. 2, 84 (1972). Structures: Woo et al., Tetrahedron Lett. 1971, 2617, 2621, 2625. Activity: Howells et al., Antimicrob. Agents Chemother. 2, 79 (1972); Heifetz et al., ibid. 89. Synthesis of butirosin B: Ikeda et al., J. Antibiot. 25, 741 (1972); Akita et al., ibid. 26, 365 (1973). Proposed biosynthetic pathway to the butirosins: K. Takeda et al., ibid. 31, 250 (1978).

Puromycin CAS Registry Number: 53-79-2 嘌呤霉素

CAS Name: 3'-[[(2S)-2-Amino-3-(4-methoxyphenyl)-1-oxopropyl]amino]-3'-deoxy-N,N-dimethyladenosine
Additional Names: L-3'-(a-amino-p-methoxyhydrocinnamamido)-3'-deoxy-N,N-dimethyladenosine; 6-di...
Literature References: Aminonucleoside antibiotic produced by the soil actinomycete Streptomyces alboniger. Structural analog of aminoacyl-tRNA; inhibits protein synthesis. Isoln: J. N. Porter et al., Antibiot. Chemother. 2, 409 (1952); eidem, US 2763642 (1956 to Am. Cyanamid). Structure: C. W. Waller et al., J. Am. Chem. Soc. 75, 2025 (1953); P. W. Fryth et al., ibid. 80, 2736 (1958). Synthesis: B. R. Baker et al., ibid. 76, 4044 (1954); 77, 12 (1955); M. J. Robins et al., J. Org. Chem. 66, 8204 (2001). Conformation: O. Jardetzky, J. Am. Chem. Soc. 85, 1823 (1963). Effect on protein synthesis: D. Nathans, Proc. Natl. Acad. Sci. USA 51, 585 (1964). Use in gene transfer studies: S. de la Luna et al., Gene 62, 121 (1988). Review: D. Nathans in Antibiotics vol. I, D. Gottlieb, P. D. Shaw, Eds. (Springer-Verlag, New York, 1967) pp 259-277.

Bunazosin CAS Registry Number: 80755-51-7 布纳唑嗪

CAS Name: 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)hexahydro-4-(1-oxobutyl)-1H-1,4-diazepine
Additional Names: 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-butyrylhexahydro-1H-1,4-diazepine; 4-ami...
Literature References: Aminoquinazoline derivative with potent hypotensive properties. Prepn: T. Takahashi, H. Sugimoto, BE 806626; eidem, US 3920636 (1974, 1975 to Eisai); alternative prepn: eidem, JP Kokai 75 140474 (1975 to Eisai), C.A. 85, 46769r (1976). In vitro and in vivo studies of adrenergic blocking action and antihypertensive properties: T. Shoji et al., Jpn. J. Pharmacol. 30, 763 (1980); K. Hoshi, S. Fujino, ibid. 427. Antihypertensive effect in volunteers: T. Kawasaki et al., Eur. J. Clin. Pharmacol. 20, 399 (1981). Pharmacokinetics: C. Yamato et al., Xenobiotica 12, 549 (1982).

Rocuronium CAS Registry Number: 143558-00-3 罗库溴胺

CAS Name: 1-[(2b,3a,5a,16b,17b)-17-(Acetyloxy)-3-hydroxy-2-(4-morpholinyl)androstan-16-yl]-1-(2-propenyl)pyrrolidinium
Additional Names: 1-allyl-1-(3a,17b-dihydroxy-2b-morpholino-5a-androstan-1...
Literature References: Aminosteroid, competitive neuromuscular blocker. Prepn: D. S. Savage et al., EP 287150; T. Sleigh et al., US 4894369 (1988, 1990 both to Akzo). Pharmacology: A. W. Muir et al., Br. J. Anaesth. 63, 400 (1989); K. Khuenl-Brady et al., Anesthesiology 72, 669 (1990). Clinical pharmacodynamics: T. J. Quill et al., Anesth. Analg. 72, 203 (1991); and pharmacokinetics in the elderly: R. S. Matteo et al., ibid. 77, 1193 (1993). Comparative clinical trial: T. Magorian et al., Anesthesiology 79, 913 (1993). HPLC determn: U. W. Kleef et al., J. Chromatogr. 621, 65 (1993). Review: T. C. Wicks, J. Am. Assoc. Nurse Anesth. 62, 33-38 (1994).

Pancuronium Bromide CAS Registry Number: 15500-66-0 泮库溴铵

CAS Name: 1,1'-[(2b,3a,5a,16b,17b)-3,17-Bis(acetyloxy)androstane-2,16-diyl]bis[1-methylpiperidinium] dibromide
Additional Names: 1,1'-(3a,17b-dihydroxy-5a-androstan-2b,16b-ylene)bis[1-methylpip...
Literature References: Aminosteroid, competitive neuromuscular blocker. Prepn: W. R. Buckett et al., Chim. Ther. 2, 186 (1967); eidem, J. Med. Chem. 16, 1116 (1973). Structural studies: Savage et al., J. Chem. Soc. B 1971, 410. Structure-activity correlation: Waser, Anaesthesist 20, 23 (1971). Pharmacology: W. R. Buckett, I. L. Bonta, Fed. Proc. 25, 718 (1966); W. R. Buckett et al., Br. J. Pharmacol. Chemother. 32, 671 (1968); I. L. Bonta et al., Eur. J. Pharmacol. 4, 83, 303 (1968). Comparative study of neuromuscular blocking and vagolytic effect: S. L. Son et al., Anesthesiology 55, 12 (1981). Review: Speight, Avery, Drugs 4, 163-226 (1972).

Vecuronium Bromide CAS Registry Number: 50700-72-6 维库溴铵

CAS Name: 1-[(2b,3a,5a,16b,17b)-3,17-Bis(acetyloxy)-2-(1-piperidinyl)androstan-16-yl]-1-methylpiperidinium bromideTrademarks: Musculax (Nippon Organon); Norcuron (Organon)
Percent Composition: ...
Literature References: Aminosteroid, competitive neuromuscular blocker. Prepn: W. R. Buckett et al., J. Med. Chem. 16, 1116 (1973); I. C. Carlyle et al., EP 8824 (1980 to Akzo), C.A. 93, 155850 (1980). Series of articles on pharmacology, pharmacokinetics, pharmacodynamics, clinical studies: Br. J. Anaesth. 52, Suppl. 1, 1S-72S (1980). Clinical pharmacology: M. R. Fahey et al., Anesthesiology 55, 6 (1981). Comparison with pancuronium bromide, q.v.: S. L. Son et al., ibid. 12.

Pipecurium Bromide CAS Registry Number: 52212-02-9 哌库溴铵

CAS Name: 4,4'-[(2b,3a,5a,16b,17b)-3,17-Bis(acetyloxy)androstane-2,16-diyl]bis(1,1-dimethylpiperazinium)dibromide
Additional Names: 4,4'-(3a,17b-dihydroxy-5a-androstan-2b,16b-ylene)bis(1,1-dime...
Literature References: Aminosteroid, competitive neuromuscular blocker. Prepn: Z. Tuba et al., DE 2337882 (1974 to Gedeon Richter), C.A. 80, 121210d (1974); Z. Tuba, Arzneim.-Forsch. 30, 342 (1980). Toxicity study: E. Kárpáti, K. Biro, ibid. 346. Series of articles on pharmacology, properties, disposition, pharmacokinetics, safety tests, clinical studies: ibid. 346-394. Determn in human serum: G. Szabo, E. Tassonyi, ibid. 31, 1013 (1981).

Vancomycin CAS Registry Number: 1404-90-6 万古霉素

Percent Composition: C 54.70%, H 5.22%, Cl 4.89%, N 8.70%, O 26.50%
Literature References: Amphoteric glycopeptide antibiotic produced by Streptomyces orientalis discovered in soil from Borneo. Inhibits bacterial cell wall synthesis by binding to peptidoglycan. Isoln: M. H. McCormick et al., Antibiot. Annu. 1955-56, 606; eidem, US 3067099 (1962 to Lilly). Pharmacology and toxicology: R. C. Anderson et al., Antibiot. Annu. 1956-57, 75. Purif: H. M. Higgins et al., ibid. 1957-58, 906. Structure studies: F. J. Marshall, J. Med. Chem. 8, 18 (1965); W. D. Weringa et al., J. Chem. Soc. Perkin Trans. 1 1972, 443; K. A. Smith et al., ibid. 1974, 2369. Total structure determination by x-ray analysis: G. M. Sheldrick et al., Nature 271, 223 (1978). Revised configuration: M. P. Williamson, D. H. Williams, J. Am. Chem. Soc. 103, 6580 (1981). Further revision of structure: C. M. Harris et al., ibid. 105, 6915 (1983). Total synthesis: K. C. Nicolaou et al., Angew. Chem. Int. Ed. 38, 240 (1999). Review of mechanism of action studies: H. P. Perkins, M. Nieto, Ann. N.Y. Acad. Sci. 235, 348-363 (1974). Series of articles on antimicrobial activity, pharmacokinetics and clinical usage: J. Antimicrob. Chemother. 14, Suppl. D, 1-109 (1984). HPLC determn in serum: L. Li et al., Ther. Drug Monit. 17, 366 (1995). Review of clinical experience: B. A. Cunha, Med. Clin. North Am. 79, 817-831 (1995).