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

Telenzepine CAS Registry Number: 80880-90-6 替仑西平

CAS Name: 4,9-Dihydro-3-methyl-4-[(4-methyl-1-piperazinylacetyl)]-10H-thieno[3,4-b][1,5]benzodiazepin-10-one
Percent Composition: C 61.60%, H 5.99%, N 15.12%, O 8.64%, S 8.66%
Literature References: Gastric secretion inhibitor; selective muscarinic M1-receptor antagonist. Prepn: V. Figala et al., EP 35519; G. Rainer, US 4381301 (1981, 1983 both to Byk-Gulden). Pharmacology: M. Eltze et al., Eur. J. Pharmacol. 112, 211 (1985). GC-MS determn in serum: E. Sturm, A. Junker, J. Chromatogr. 430, 43 (1988). Clinical pharmacology: W. Londong et al., Gut 28, 888 (1987); R.W. Stockbrügger et al., Z. Gastroenterol. 26, 297 (1988). Comparative clinical trial with ranitidine: B. Simon et al., ibid. 28, 90 (1990).

Zolimidine CAS Registry Number: 1222-57-7 佐利米定

CAS Name: 2-[4-(Methylsulfonyl)phenyl]imidazo[1,2-a]pyridine
Additional Names: zoliridine
Trademarks: Solimidin (Selvi)
Percent Composition: C 61.75%, H 4.44%, N 10.29%, O 11.75%, S 11.77...
Literature References: Gastroprotective agent. Prepn: GB 991589; L. Almirante et al., US 3318880 (1965, 1967 both to Selvi); eidem, J. Med. Chem. 8, 305 (1965). Metabolism: eidem, Farmaco Ed. Sci. 29, 941 (1974). Series of articles on pharmacology: Panminerva Med. 16, 301-359 (1974). Pharmacokinetics: E. Schraven, D. Trottnow, Arzneim.-Forsch. 26, 213 (1976). Clinical mucopoietic activity: S. Abate et al., Int. J. Tissue React. 4, 319 (1982); M. C. Parodi et al., Scand. J. Gastroenterol. 19, Suppl. 92, 163 (1984). Clinical study: A. Materia et al., Clin. Ter. 97, 183 (1981).

Pentolinium Tartrate CAS Registry Number: 52-62-0 3-溴-4-氟甲苯

CAS Name: 1,1'-(1,5-Pentanediyl)bis[1-methylpyrrolidinium] salt with (2R,3R)-2,3-dihydroxybutanedioic acid (1:2)
Additional Names: pentamethylene-1,5-bis(1-methylpyrrolidinium) hydrogen tartrat...
Literature References: General procedure of prepn: Libman et al., J. Chem. Soc. 1952, 2305. Ganglionic blocking agent.

Micronomicin CAS Registry Number: 52093-21-7 小诺米星

CAS Name: O-2-Amino-2,3,4,6-tetradeoxy-6-(methylamino)-a-D-erythro-hexopyranosyl-(1®4)-O-[3-deoxy-4-C-methyl-3-(methylamino)-b-L-arabinopyranosyl-(1®6)]-2-deoxy-D-streptamine
Additional Names: ...
Literature References: Gentamicin C complex antibiotic produced by Micromonospora sagamiensis var. nonreducans: T. Nara et al., DE 2326781 (1973 to Kyowa), C.A. 80, 58389b (1974); eidem, US 4045298 (1977 to Abbott). Isoln, physicochemical and antibacterial properties: R. Okachi et al., J. Antibiot. 27, 793 (1974). Structure: R. S. Egan et al., ibid. 28, 29 (1975). Identity with gentamicin C2b: P. J. L. Daniels et al., ibid. 35. Pharmacology: T. Hashimoto et al., Jpn. J. Antibiot. 30, 362 (1977), C.A. 89, 17113z (1978). Toxicity studies: T. Hara et al., ibid. 386-449, C.A. 89, 209205c-8f (1978). Biosynthesis: H. Kase et al., J. Antibiot. 35, 1 (1982); eidem, Agric. Biol. Chem. 46, 515 (1982). Series of articles on pharmacology, metabolism and clinical studies: Chemotherapy (Tokyo) 25, 1801-2287 (1977). See also Gentamicin.

Sisomicin CAS Registry Number: 32385-11-8 西索米星

CAS Name: O-3-Deoxy-4-C-methyl-3-(methylamino)-b-L-arabinopyranosyl-(1®6)-O-[2,6-diamino-2,3,4,6-tetradeoxy-a-D-glycero-hex-4-enopyranosyl-(1®4)]-2-deoxy-D-streptamine
Additional Names: (2S-cis...
Literature References: Gentamicin-like aminoglycoside antibiotic produced by Micromonospora inyoesis (NRRL 3292): M. J. Weinstein et al. DE 1932309; eidem, US 3832286 (1970, 1974 both to Schering); eidem, J. Antibiot. 23, 551 (1970). Isoln: G. H. Wagman et al., ibid. 555. Chemical and physical studies: Cooper et al., Chem. Commun. 1971, 285, 924; Kugelman et al., J. Antibiot. 26, 394 (1973). Structure consists of 2-deoxystreptamine, q.v., linked to two saccharide units, garosamine and sisosamine: Keiman et al., J. Org. Chem. 39, 1451 (1974). Synthesis: D. H. Davies et al., J. Med. Chem. 21, 189 (1978). Synthesis of sisosamine derivs: Cleophax et al., Chem. Commun. 1975, 11. Has broad spectrum antibiotic activity: Waitz et al., J. Antibiot. 23, 559 (1970). Biotransformation of sisomicin to gentamicin: B. K. Lee et al., Antimicrob. Agents Chemother. 12, 335 (1977). Clinical studies: R. Lorber et al., Clin. Ther. 4, 263 (1981); J. P. Sculier et al., J. Antimicrob. Chemother. 9, 63 (1982). Review: P. Noone, Drugs 27, 548-578 (1984).

Beclomethasone CAS Registry Number: 4419-39-0 倍氯米松

CAS Name: (11b,16b)-9-Chloro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione
Additional Names: 9a-chloro-16b-methyl-1,4-pregnadiene-11b,17a,21-triol-3,20-dione; 9a-chloro-16b-methylpre...
Literature References: Glucocorticoid. Prepn of free alcohol and 21-acetate: GB 912378 (1962 to Merck Co.); of 21-acetate: GB 901093 (1962 to Schevico); of mono and diesters: J. Elks et al., BE 649170; eidem, US 3312590 (1964, 1967 both to Glaxo). Symposium on clinical studies: Br. J. Clin. Pharmacol. 4, Suppl. 3, 249S-312S (1977). Use in chronic asthma in children: M. Rao et al., J. Asthma 19, 21 (1982); in treatment of asthma in steroid-independent adults: V. A. Malfitan, Clin. Ther. 4, 472 (1982). Review of use in rhinitis: P. Small et al., Ann. Allergy 49, 127 (1982); of pharmacology, side effects and use in asthma and allergic rhinitis: R. N. Brogden et al., Drugs 28, 99-126 (1984).

Glufosfamide CAS Registry Number: 132682-98-5 葡磷酰胺

CAS Name: 1-[N,N'-Bis(2-chloroethyl)phosphorodiamidate]-b-D-glucopyranose
Additional Names: b-D-glucopyranosyl N,N'-di(2-chloroethyl) phosphoric acid diamide; b-D-glucosylisophosphoramide musta...
Literature References: Glucose coupled to isophosphoramide mustard, the active metabolite of the alkylating agent ifosfamide, q.v. Enters cells through upregulated glucose transport proteins. Prepn: M. Wiessler, M. Dickes, DE 3835772; eidem, US 5622936 (1990, 1997 both to Deutsches Krebsforschungszentrum Stiftung). Pharmacology and toxicity studies: J. Pohl et al., Cancer Chemother. Pharmacol. 35, 364 (1995). Mechanism of action study: H. Seker et al., Br. J. Cancer 82, 629 (2000). Clinical evaluation in pancreatic cancer: E. Briasoulis et al., Eur. J. Cancer 39, 2334 (2003); in non-small cell lung cancer: G. Giaccone et al., ibid. 40, 667 (2004). Review of pharmacology and clinical development: I. Niculescu-Duvaz, Curr. Opin. Invest. Drugs 3, 1527-1532 (2002).

Carminic Acid CAS Registry Number: 1260-17-9 胭脂红酸

CAS Name: 7-a-D-Glucopyranosyl-9,10-dihydro-3,5,6,8-tetrahydroxy-1-methyl-9,10-dioxo-2-anthracenecarboxylic acid
Additional Names: C.I. Natural Red 4; C.I. 75470
Percent Composition: C 53.66...
Literature References: Glucosidal coloring matter from the scale insect Coccus cacti L., Homoptera (cochineal). The essential constituent of carmine. Isoln: Schunk, Marchlewski, Ber. 27, 2979 (1894); Dimroth, Scheuer, Ann. 399, 43 (1913). Structure: Dimroth, Kammerer, Ber. 53, 471 (1920); Ali, Haynes, J. Chem. Soc. 1959, 1033; revised structure: Bhatia, Venkataraman, Indian J. Chem. 3 (2), 92 (1965). See also Colour Index vol. 4 (3rd ed., 1971) p 4632.

Colocynthin CAS Registry Number: 1398-78-3 alpha-西洋苦瓜素2-D-吡喃葡萄糖苷

CAS Name: 25-(Acetyloxy)-2-(b-D-glucopyranosyloxy)-16,20-dihydroxy-9-methyl-19-norlanosta-1,5,23-triene-3,11,22-trione
Additional Names: 2-O-b-D-glucopyranosylcucurbitacin E
Percent Composit...
Literature References: Glucoside from fruit of Citrullus colocynthis Schrad., Cucurbitaceae: Walz, Neues Jahrb. Pharm. 9, 16, 225 (1858); 16, 10 (1861); Henke, Arch. Pharm. 221, 200 (1883); Naylas, Chappel, Pharm. J. 25, 117 (1907); Lavie et al., Acta Univ. Int. Contra Cancerum 15, 177 (1959); Khadem, Rahman, Tetrahedron Lett. 1962, 1137. Other isolns: H. Ripperger, K. Seifert, Tetrahedron 31, 1561 (1975); H. Ripperger, ibid. 32, 1567 (1976). Structure: Khadem, Rahman, J. Chem. Soc. 1963, 4991.

Pseudojervine CAS Registry Number: 36069-05-3 假白藜芦碱

CAS Name: (3b,23b)-17,23-Epoxy-3-(b-D-glucopyranosyloxy)veratraman-11-one
Percent Composition: C 67.44%, H 8.40%, N 2.38%, O 21.78%
Literature References: Glucoside of jervine. Isoln from Veratrum album L., Liliaceae: Wright, Luff, J. Chem. Soc. 35, 405 (1879); Poethke, Arch. Pharm. 276, 170 (1938); from V. viride Ait., Liliaceae: Jacobs, Craig, J. Biol. Chem. 155, 565 (1944); from V. eschscholtzii Gray, Liliaceae: Klohs et al., J. Am. Chem. Soc. 75, 2133 (1953).