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

Cinromide CAS Registry Number: 58473-74-8 反式-3-溴-N-乙基肉桂酰胺

CAS Name: (2E)-3-(3-Bromophenyl)-N-ethyl-2-propenamide
Additional Names: trans-3-bromo-N-ethylcinnamamideTrademarks: Vumide (Burroughs Wellcome)
Percent Composition: C 51.99%, H 4.76%, Br 31...
Literature References: Cinnamic acid derivative with anti-epileptic activity. Prepn: E. M. Grivsky, DE 2535599; idem, US 4041071 (1976, 1977 to Burroughs Wellcome). Pharmacology: F. E. Soroko et al., J. Pharm. Pharmacol. 33, 741 (1981); G. H. Fromm et al., Epilepsia 24, 394 (1983). Pharmacokinetics and metabolism: R. R. Maddox, B. B. Wannamaker, Curr. Ther. Res. 32, 165 (1982). Mass spec determn in plasma and urine: R. J. Perchalski et al., Anal. Chem. 54, 1466 (1982). Controlled clinical trials: J. W. Allen et al., Epilepsia 24, 422 (1983); B. Spilker et al., Curr. Ther. Res. 34, 7 (1983).

DIDS CAS Registry Number: 53005-05-3 4,4′-二异硫氰酰-2,2′-基二磺酸二钠盐

CAS Name: 2,2'-(1,2-Ethenediyl)bis[5-isothiocyanatobenzenesulfonic acid]
Additional Names: 4,4'-diisothiocyanato-2,2'-stilbenedisulfonic acid
Percent Composition: C 42.28%, H 2.22%, N 6.16%,...
Literature References: Classic inhibitor of ion transport across biological membranes. Prepn: Z. I. Cabantchik, A. Rothstein, J. Membr. Biol. 10, 311 (1972); of tritated form: S. Ship et al., ibid. 33, 311 (1977). Inhibition of chloride transport: T. Janas et al., Am. J. Physiol. 257, C601 (1989); J.-A. Kim et al., Biochem. Biophys. Res. Commun. 309, 291 (2003); of non-selective cation conductance: A. Diakov et al., Pflugers Arch. Eur. J. Physiol. 442, 700 (2001). Effects of ionic strength and pH on membrane penetration: V. A. Tverdislov et al., Colloids Surfaces B 5, 205 (1995). Mechanism of inhibition in erythrocytes: J. M. Salhany, Blood Cells Mol. Dis. 27, 901 (2001); of cardiac ryanodine receptor: A. P. Hill, R. Sitsapesan, Biophys. J. 82, 3037 (2002).

Dodecahedrane CAS Registry Number: 4493-23-6 正十二面烷

CAS Name: Hexadecahydro-5,2,1,6,3,4-[2,3]butanediyl[1,4]diylidenedipentaleno[2,1,6-cde:2',1',6'-gha]pentalene
Additional Names: pentagonal dodecahedrane
Percent Composition: C 92.26%, H 7.74...
Literature References: Classical uniform convex polyhedrane. Theoretical studies: O. Ermer, Angew. Chem. Int. Ed. 16, 411 (1977); R. L. Disch, J. M. Schulman, J. Am. Chem. Soc. 103, 3297 (1981). Review of synthetic studies: P. E. Eaton, Tetrahedron 35, 2189-2223 (1979). Total synthesis: R. J. Ternansky et al., J. Am. Chem. Soc. 104, 4503 (1982).

Cuproxoline CAS Registry Number: 13007-93-7

CAS Name: Tetrahydrogen bis[8-hydroxy-5,7-quinolinedisulfonato(3-)-N1,O8]cuprate(4-) compd with N-ethylethanamine (1:4)
Additional Names: 8-hydroxy-5,7-quinolinedisulfonic acid copper derivativ...
Literature References: Clinical efficacy in treatment of arthritis: W. C. Kuzell et al., Ann. Rheum. Dis. 10, 328 (1951). Veterinary use as parenteral copper supplement: I. J. Cunningham, N. Z. Vet. J. 7, 15 (1959); N. F. Suttle, Vet. Rec. 109, 304 (1981); G. J. Judson et al., Aust. Vet. J. 61, 40 (1984). Review of use of organic copper complexes in treatment of rheumatoid and degenerative diseases: J. R. J. Sorenson, W. Hangarter, Inflammation 2, 217-238 (1977). Review of veterinary use: W. M. Allen, C. B. Mallinson, Vet. Rec. 114, 451-454 (1984).

Diprenorphine CAS Registry Number: 14357-78-9 地利洛非

CAS Name: (5a,7a)-17-(Cyclopropylmethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-a,a-dimethyl-6,14-ethenomorphinan-7-methanol
Additional Names: 21-cyclopropyl-6,7,8,14-tetrahydro-7a-(1-hydr...
Literature References: Closely related to cyprenorphine, q.v. Prepn: K. W. Bentley, D. G. Hardy, J. Am. Chem. Soc. 89, 3281 (1967). Activity in rats: G. F. Blane, J. Pharm. Pharmacol. 19, 367 (1967); G. F. Blane, D. Dugdall, ibid. 20, 547 (1968). Use as etorphine antagonist in dogs: M. Grange et al., Rev. Med. Vet. 124, 899 (1973); in large animals: B. T. Alford et al., J. Am. Vet. Med. Assoc. 164, 702 (1974). Binding to opiate receptors: C. B. Pert et al., Life Sci. 16, 1849 (1975); J. Pearson et al., ibid. 26, 1047 (1980); to m opiate receptors: J. J. Frost et al., ibid. 38, 1597 (1986). Treatment of experimental stroke in cats: D. S. Baskin et al., Neuropeptides 5, 307 (1985); eidem, J. Neurosurg. 64, 99 (1986). Determn by HPLC: I. Jane, A. McKinnon, J. Chromatogr. 323, 191 (1985). Toxicity data: N. S. Duggett et al., Toxicol. Appl. Pharmacol. 31, 141 (1977).

Gelsemine CAS Registry Number: 509-15-9 钩吻素甲

Percent Composition: C 74.51%, H 6.88%, N 8.69%, O 9.93%
Literature References: CNS stimulant from roots and rhizome of Gelsemium sempervirens (L.) Ait., Loganiaceae. Isoln: Gerrard, Pharm. J. 13, 641 (1883); Moore, J. Chem. Soc. 97, 2223 (1910); 99, 1231 (1911); Sayre, Watson, J. Am. Pharm. Assoc. 8, 708 (1919); Chou, Chin. J. Physiol. 5, 131 (1931), C.A. 25, 40856 (1931); Schwarz, Marion, Can. J. Chem. 31, 958 (1953). Structure: Conroy, Chakrabarti, Tetrahedron Lett. 1959 (4), 6; Lovell et al., ibid. 1; Roe, Gates, Tetrahedron 11, 148 (1960). NMR spectroscopic study: Y. Schun, G. A. Cordell, J. Nat. Prod. 48, 969 (1985). Partial syntheses: W. E. Earley et al., Tetrahedron Lett. 29, 3781, 3785 (1988).

Harmaline CAS Registry Number: 304-21-2 骆驼蓬灵

CAS Name: 4,9-Dihydro-7-methoxy-1-methyl-3H-pyrido[3,4-b]indole
Additional Names: 1-methyl-7-methoxy-3,4-dihydro-b-carboline; 3,4-dihydroharmine; harmidine; harmalol methyl ether; O-methylharma...
Literature References: CNS stimulant from seeds of Peganum harmala L., Zygophyllaceae: Goebel, Ann. 38, 363 (1841); from Banisteria caapi Spruce, Malpighiaceae: Hochstein, Paradies, J. Am. Chem. Soc. 79, 5735 (1957). Structure: Manske et al., J. Chem. Soc. 1927, 1. Synthesis: Späth, Lederer, Ber. 63, 120, 2102 (1930); Spenser, Can. J. Chem. 37, 1851 (1959). Identity with harmidine: Robinson, Chem. Ind. (London) 1965, 605. Pharmacology: Fuentes, Longo, Neuropharmacology 10, 15 (1971). Metabolism: Ho et al., Biochem. Pharmacol. 20, 1313 (1971). Review of structure and synthesis work: Hofmann, Sven. Farm. Tidskr. 75, 933 (1971), C.A. 76, 149609g (1972).

Harmine CAS Registry Number: 442-51-3 哈尔碱; 哈尔明碱; 肉叶云香碱; 去氢骆驼蓬碱

CAS Name: 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole
Additional Names: banisterine; yageine; telepathine; leucoharmine
Percent Composition: C 73.56%, H 5.70%, N 13.20%, O 7.54%
Literature References: CNS stimulant isolated from seeds of Peganum harmala L., Zygophyllaceae: Göbel, Ann. 38, 363 (1841); Reinhard et al., Phytochemistry 7, 503 (1968); from Banisteria caapi Spruce, Malpighiaceae: Hochstein, Paradies, J. Am. Chem. Soc. 79, 5735 (1957); from Banisteriopsis inebrians Morton, Malpighiaceae: O'Connell, Lynn, J. Am. Pharm. Assoc. 42, 753 (1953). Structure: Manske et al., J. Chem. Soc. 1927, 1, 240. Synthesis: Späth, Lederer, Ber. 63B, 120 (1930); Akaboro, Saito, ibid. 2245; Hahn et al., Ber. 67B, 2031 (1934), Ann. 520, 107, 123 (1935), Ber. 71B, 2163, 2175 (1938); Harvey, Robson, J. Chem. Soc. 1938, 97. Metabolism: Slotkin, DiStefano, J. Pharmacol. Exp. Ther. 174, 456 (1970). Toxicity study: K. K. Chen et al., J. Pharmacol. Exp. Ther. 79, 127 (1943).

Prodipine CAS Registry Number: 31314-38-2 普罗地平

CAS Name: 1-(1-Methylethyl)-4,4-diphenylpiperidine
Additional Names: 1-isopropyl-4,4-diphenylpiperidine
Percent Composition: C 85.97%, H 9.02%, N 5.01%
Literature References: CNS stimulating agent with antidepressant and antiparkinson properties. Prepn: H. G. Menge, J. Klosa, DE 1936452; eidem, US 4016280 (1971, 1977 both to Byk Gulden). Evaluation of MAO-inhibitory properties in vivo and in vitro: G. Planz et al., Arzneim.-Forsch. 23, 281 (1973). Effects on 5-hydroxytryptamine uptake in platelets: M. Eltze et al., ibid. 30, 1129 (1980). Comparative study of effects in Parkinson's disease: E. Gründig, F. Gerstenbrand, Wien. Klin. Wochenschr. 92, 868 (1980).

IACFT CAS Registry Number: 180468-34-2 (1R,2S,3S,5S)-3-(4-氟苯基)-8-[(E)-3-碘丙-2-烯基]-8-氮杂双环[3.2.1]辛烷-2-羧酸甲酯

CAS Name: (1R,2S,3S,5S)-3-(4-Fluorophenyl)-8-[(2E)-3-(iodo-2-propenyl)]-8-azabicyclo[3.2.1]octane-2-carboxylic acid methyl ester
Additional Names: 2b-carboxymethoxy-3b-(4-fluorophenyl)-N-(1-iod...
Literature References: Cocaine analog with dopamine transport inhibitor activity. Radiolabeled form designed for SPECT brain imaging. Prepn: D. R. Elmaleh et al.,WO 9511901; eidem, US 5493026 (1995, 1996 both to Gen. Hosp. Corp., Harvard College, Organix and Northeastern Univ.); and receptor binding studies: eidem, J. Nucl. Med. 37, 1197 (1996). Series of articles on pharmacology and binding studies: B. K. Madras et al., Synapse 29, 93-127 (1998). Clinical evaluation in Parkinson's disease: A. J. Fischman et al., ibid. 128. CE determn in plasma: K. Hettiarachchi et al., J. Chromatogr. A 895, 87 (2000).