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

Gougerotin CAS Registry Number: 2096-42-6 b-D-葡萄吡喃氨基,1-(4-氨基-2-氧-1(2H)-嘧啶酰)-1,4-去二氧-4-[(N-甲基甘基-D-丝基)氨基]-

CAS Name: 1-(4-Amino-2-oxo-1(2H)-pyrimidinyl)-1,4-dideoxy-4-[[N-(N-methylglycyl)-D-seryl]amino]-b-D-glucopyranuronamide
Additional Names: 1-(4-amino-2-oxo-1(2H)-pyrimidinyl)-1,4-dideoxy-4-[D-2-...
Literature References: Antibiotic substance with antibacterial and antineoplastic activity. Isoln from Streptomyces gougerotii: Kanzaki et al., J. Antibiot. 15A, 93 (1962). Identity with asteromycin: Ikeuchi et al., ibid. 25, 548 (1972). Structure: Iwasaki, Yakugaku Zasshi 82, 1358 (1962). Revised structure: Fox et al., Tetrahedron Lett. 1968, 6029; Watanabe et al., Chem. Pharm. Bull. 17, 416 (1969). Total synthesis: eidem, J. Am. Chem. Soc. 94, 3272 (1972); Lichtenthaler et al., Tetrahedron Lett. 1975, 3527. Identity with aspiculamycin: Lichtenthaler et al., ibid. 665. Mechanism of action study: J. C. Lacal et al., J. Antibiot. 33, 441 (1980). Reviews: Clark in Antibiotics vol. 1, D. Gottlieb, P. D. Shaw, Eds. (Springer-Verlag, New York, 1967) pp 278-282; Yukioka, ibid. vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (1975) pp 448-458.

Stallimycin CAS Registry Number: 636-47-5 司他霉素

CAS Name: N-[5-[[(3-Amino-3-iminopropyl)amino]carbonyl]-1-methyl-1H-pyrrol-3-yl]-4-[[[4-(formylamino)-1-methyl-1H-pyrrol-2-yl]carbonyl]amino]-1-methyl-1H-pyrrole-2-carboxamide
Additional Names:...
Literature References: Antibiotic substance with antiviral and oncolytic properties, obtained from Streptomyces distallicus: Arcamone et al., DE 1039198 (1958 to Farmaceutici Italia), C.A. 55, 2012f (1961). Structure and synthesis: Arcamone et al., Nature 203, 1064 (1964); eidem, Gazz. Chim. Ital. 97, 1097, 1110 (1967). Total synthesis: M. Bialer et al., Tetrahedron 1978, 2389; L. Grehn, U. Ragnarsson, J. Org. Chem. 46, 3492 (1981). Toxicity and antitumor activity: A. DiMarco et al., Cancer Chemother. Rep. 18, 15 (1962). Review: Hahn in Antibiotics vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (Springer-Verlag, New York, 1975) pp 79-100.

Fusafungine CAS Registry Number: 1393-87-9 夫沙芬净

Trademarks: Biofusal; Fusaloyos; Fusarine; Locabiotal (Servier)
Literature References: Antibiotic used as an aerosol for local application. Isoln from Fusarium species: Couchoud, FR 1164181 (1958), C.A. 54, 20074b (1960); Servier, BE 612474 (1962), C.A. 57, 11320b (1962); idem, GB 1018626 (1966 to Biofarma), C.A. 64, 16585b (1966). Bacteriological activity: D. Haler, J. Int. Med. Res. 5, 61 (1977); idem, Vie Med. 61, 507 (1980).

Mofarotene CAS Registry Number: 125533-88-2 莫法罗汀

CAS Name: 4-[2-[4-[(1E)-2-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl]phenoxy]ethyl]morpholinePercent Composition: C 80.32%, H 9.07%, N 3.23%, O 7.38%
Literature References: Anticancer aromatic analog of retinoic acid (arotinoid). Prepn: M. Klaus et al., EP 331983; eidem, US 4940707 (1989, 1990 both to Hoffmann-La Roche). Mode of action study: J. F. Eliason et al., Blood 86, 4516 (1995). Pharmacokinetics: B. Vallès et al., Eur. J. Drug Metab. Pharmacokinet. 20, 49 (1995). HPLC determn in plasma: R. Wyss et al., J. Chromatogr. A 729, 315 (1996). Mechanism of growth inhibition on pancreatic cancer cells: S. Kawa et al., Int. J. Cancer 72, 906 (1997). Clinical pharmacology in combination with cisplatin and etoposide: L. van Zuylen et al., Anti-Cancer Drugs 10, 361 (1999).

Flutropium Bromide CAS Registry Number: 63516-07-4 氟托溴铵

CAS Name: (endo,syn)-8-(2-Fluoroethyl)-3-[(hydroxydiphenylacetyl)oxy]-8-methyl-8-azoniabicyclo[3.2.1]octane bromide
Additional Names: (8r)-3a-benziloyloxy-8-(2-fluoroethyl)-8-methyl-8-azoniabic...
Literature References: Anticholinergic agent. Prepn: R. Banholzer et al., DE 2540633; eidem, US 4042700 (both 1977 to Boehringer, Ing.). Synthesis: R. Banholzer et al., Arzneim.-Forsch. 36, 1161 (1986). Molecular and crystal structure: G. Kiel, ibid. 1166. Pharmacology in animals: S. Yanaura et al., Jpn. J. Pharmacol. 33, 971 (1983); R. Bauer, A. Fügner, Arzneim.-Forsch. 36, 1348 (1986). Pharmacodynamics: K. Yoshimura et al., Iyakuhin Kenkyu 18, 240 (1987), C.A. 107, 17197v (1987).

Etomidoline CAS Registry Number: 21590-92-1 依托多林

CAS Name: 2-Ethyl-2,3-dihydro-3-[[4-[2-(1-piperidinyl)ethoxy]phenyl]amino]-1H-isoindol-1-one
Additional Names: 2-ethyl-3-(b-piperidino-p-phenetidino)phthalimidineTrademarks: Smedolin (Yamanouch...
Literature References: Anticholinergic antispasmodic. Prepn: N. Giraldi, V. Mariotti, ZA 6705704; eidem, US 3624206 (1968, 1971 both to Erba). Quantitative evaluation in humans: G. Sacchetti et al., Farmaco Ed. Prat. 27, 708 (1972). Spasmolytic properties: M. Takeda, Oyo Yakuri 7, 903 (1973), C.A. 80, 66678 (1974). Pharmacology: M. Takeda et al., ibid. 1073, C.A. 81, 33285 (1974); T. Mukai et al., Jpn. J. Pharmacol. 31, 147 (1981), C.A. 95, 18068 (1981).

Oxitropium Bromide CAS Registry Number: 30286-75-0 氧托溴铵

CAS Name: [7(S)-(1a,2b,4b,5a,7b)]-9-Ethyl-7-(3-hydroxy-1-oxo-2-phenylpropoxy)-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide
Additional Names: (8r)-6b,7b-epoxy-8-ethyl-3a-hydroxy-1aH...
Literature References: Anticholinergic bronchodilating agent. Prepn: K. Zeile et al., US 3472861 (1969 to Boehringer, Ing.). Comparison with fenoterol, q.v.: D. Nolte, Respiration 36, 32 (1978); with ipratropium bromide, q.v.: J. Lulling et al., ibid. 42, 188 (1981). Efficacy in bronchial asthma: H. M. Beumer et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 19, 168 (1981); in exercise-induced asthma: K. Larsson, Respiration 43, 57 (1982).

Scopolamine CAS Registry Number: 51-34-3 东莨菪碱

CAS Name: (aS)-a-(Hydroxymethyl)benzeneacetic acid (1a,2b,4b,5a,7b)-9-methyl-3-oxa-9-azatricyclo[3.3.1.02,4]non-7-yl ester
Additional Names: 6b,7b-epoxy-1aH,5aH-tropan-3a-ol (-)-tropate; 6b,7b-...
Literature References: Anticholinergic, tropane alkaloid isolated from Datura metel L., Scopola carniolica Jacq. and other Solanaceae. Constituent of impure duboisine from Duboisia myoporoides R. Br., pure duboisine is l-hyoscyamine, q.v. Isoln: A. Ladenburg, Ann. 206, 274 (1881); E. Schmidt, Arch. Pharm. 230, 207 (1892). Identity with hyoscine: O. Hesse, Ann. 271, 100 (1892); idem, J. Prakt. Chem. 66, 194 (1902). Absorption spectra: J. J. Dobbie, J. J. Fox, J. Chem. Soc. 103, 1194 (1913). Resolution of isomers and review of early literature: H. King, ibid. 1919, 476. Extraction procedure: F. Chemnitius, J. Prakt. Chem. 120, 221 (1928). Structural studies: J. Gadamer, F. Hammer, Arch. Pharm. 259, 122 (1921); K. Hess, O. Wahl, Ber. 55, 1979 (1922); R. Willstätter, E. Berner, ibid. 56, 1079 (1923); W. Steffens, Arch. Pharm. 262, 205 (1924). Configuration: G. Fodor, Nature 170, 278 (1952); J. Meinwald, J. Chem. Soc. 1953, 712. Review of stereochemistry: G. Fodor, Tetrahedron 1, 86 (1957). Absolute configuration of tropic acid moiety: G. Fodor, G. Csepreghy, Tetrahedron Lett. 1959, 16; eidem, J. Chem. Soc. 1961, 3222. Synthesis of DL-form: G. Fodor et al., Chem. Ind. (London) 1956, 764; P. Dobo et al., J. Chem. Soc. 1959, 3461. Clinical evaluation in motion sickness: J. J. Brand, P. Whittingham, Lancet 2, 232 (1970); in peripheral vertigo: T. Rahko, P. Karma, J. Laryngol. Otol. 99, 653 (1985). Acute toxicity of the hydrobromide: Stockhaus, Wick, Arch. Int. Pharmacodyn. Ther. 180, 155 (1969). Review of CNS effects in humans: D. J. Safer, R. P. Allen, Biol. Psychiatry 3, 347-355 (1971); of use in anesthesia: L. E. Shutt, J. B. Bowles, Anaesthesia 34, 476-490 (1979); of pharmacology and clinical efficacy: S. P. Clissold, R. C. Heel, Drugs 29, 189-207 (1985). Comprehensive description: F. J. Muhtadi, M. M. A. Hassan, Anal. Profiles Drug Subs. 19, 477-551 (1990).

Hexocyclium Methyl Sulfate CAS Registry Number: 115-63-9 甲硫己环铵

CAS Name: 4-(2-Cyclohexyl-2-hydroxy-2-phenylethyl)-1,1-dimethylpiperazinium methyl sulfate (salt)
Additional Names: N-(b-cyclohexyl-b-hydroxy-b-phenylethyl)-N1-methylpiperazine methosulfate; N-...
Literature References: Anticholinergic. Description: Helgren et al., J. Am. Pharm. Assoc. Sci. Ed. 46, 639 (1957). Prepn: Weston, US 2907765 (1959 to Abbott).

Hyoscyamine CAS Registry Number: 101-31-5 天仙子胺

CAS Name: [3(S)-endo]-a-(Hydroxymethyl)benzeneacetic acid 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
Additional Names: 1aH,5aH-tropan-3a-ol(-)-tropate (ester); 3a-tropanyl S-(-)-tropate; l-trop...
Literature References: Anticholinergic. From Hyoscyamus niger L., Atropa belladonna L., Datura stramonium L., and other Solanaceae: Ladenburg, Ann. 206, 274 (1881). Identity with duboisine and daturine: Beckurts, Apoth. Ztg. 27, 683 (1912). Obtained by resolution of atropine: Werner, Miltenberger, Ann. 631, 163 (1960). Prepd from (-)-acetyltropoyl chloride and atropine hydrochloride: Fodor et al., Acta Chim. Acad. Sci. Hung. 28(4), 409 (1961), C.A. 61, 1903g (1964). Configuration: Fodor, Csepreghy, Tetrahedron Letters no. 7, 16 (1959). Comprehensive description: F. J. Muhtadi, Anal. Profiles Drug Subs. Excip. 23, 153-228 (1994).