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

Venlafaxine CAS Registry Number: 93413-69-5 D,L-文拉法辛

CAS Name: 1-[2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol
Additional Names: (±)-1-[a-[(dimethylamino)methyl]-p-methoxybenzyl]cyclohexanol; N,N-dimethyl-2-(1-hydroxycyclohexyl)-2...
Literature References: Serotonin noradrenaline reuptake inhibitor (SNRI). Prepn: G. E. M. Husbands et al., EP 112669; US 4535186 (1984, 1985 both to Am. Home Prods.); and resolution of isomers: J. P. Yardley et al., J. Med. Chem. 33, 2899 (1990). Receptor binding studies: E. A. Muth et al., Biochem. Pharmacol. 35, 4493 (1986). HPLC determn in biological fluids: D. R. Hicks et al., Ther. Drug Monit. 16, 100 (1994). Clinical pharmacokinetics: K. J. Klamerus et al., J. Clin. Pharmacol. 32, 716 (1992). Clinical trial in major depression: E. Schweizer et al., J. Clin. Psychopharmacol. 11, 233 (1991). Review of pharmacology and clinical efficacy in depression: S. A. Montgomery, J. Clin. Psychiatry 54, 119-126 (1993). Clinical trial in generalized anxiety disorder: A. J. Gelenberg et al., J. Am. Med. Assoc. 283, 3082 (2000).

Renzapride CAS Registry Number: 112727-80-7 伦扎必利

CAS Name: rel-4-Amino-N-(1R,4S,5R)-1-azabicyclo[3.3.1]non-4-yl-5-chloro-2-methoxybenzamide
Additional Names: (±)-endo-4-amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamidePer...
Literature References: Serotonin receptor 5-HT4 agonist/5-HT3 antagonist. Prepn: F. D. King, EP 94742; idem, US 4612319 (1983, 1986 both to Beecham); idem et al., J. Med. Chem. 36, 683 (1993). 5-HT4 receptor selectivity as quaternary salt: G. S. Baxter et al., Bioorg. Med. Chem. Lett. 3, 633 (1993). Clinical pharmacology: D. H. Staniforth, M. Pennick, Eur. J. Clin. Pharmacol. 38, 161 (1990). Clinical evaluation in irritable bowel syndrome: M. Camilleri et al., Clin. Gastroenterol. Hepatol. 2, 895 (2004). Review: P. Norman, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 2, 355-368 (2000).

Methysergide CAS Registry Number: 361-37-5 美西麦角

CAS Name: (8b)-9,10-Didehydro-N-[(1S)-1-(hydroxymethyl)propyl]-1,6-dimethylergoline-8-carboxamide
Additional Names: N-[1-(hydroxymethyl)propyl]-1-methyl-D-lysergamide; 1-methylmethylergonovine;...
Literature References: Serotonin receptor antagonist. Prepn: GB 854569 (1960); A. Hofmann, F. Troxler, US 3113133 (1963 to Sandoz). Comparative pharmacology: Z. Votava et al., Arzneim.-Forsch. 16, 220 (1966); P. N. Chambers, P. B. Marshall, J. Pharm. Pharmacol. 19, 65 (1967). Mechanism of action: D. A. Curran et al., Res. Clin. Stud. Headache 1, 74 (1967); J. E. Hardebo et al., Neurology 28, 64 (1978); S. W. J. Lamberts, R. M. Mac Leod, Endocrinology 103, 287 (1978).

Mianserin CAS Registry Number: 24219-97-4 米安舍林

CAS Name: 1,2,3,4,10,14b-Hexahydro-2-methyldibenzo[c,f]pyrazino[1,2-a]azepine
Additional Names: 2-methyl-1,2,3,4,10,14b-hexahydro-2H-pyrazino[1,2-f]morphanthridine
Percent Composition: C 81....
Literature References: Serotonin receptor antagonist. Prepn: NL 6603256; van der Burg, Delobelle, US 3534041 (1967, 1970, both to Organon); van der Burg et al., J. Med. Chem. 13, 35 (1970). Pharmacology: Saxena et al., Eur. J. Pharmacol. 13, 295 (1971); Vargaftig et al., ibid. 16, 336 (1971); Van Riezen, Arch. Int. Pharmacodyn. Ther. 198, 256 (1972). Molecular and crystal structure: van Rij, Feil, Tetrahedron 29, 1891 (1973). Review of pharmacology and therapeutic efficacy in depressive illness: R. N. Brogden et al., Drugs 16, 273-301 (1978). 5HT-receptor binding study: B. S. Alexander, M. D. Wood, J. Pharm. Pharmacol. 39, 664 (1987). Review: H. van Riezen et al., in Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 56-93; Br. J. Clin. Pharmacol. 15, Suppl. 2, S141-S342 (1983).

Clomipramine CAS Registry Number: 303-49-1 氯米帕明

CAS Name: 3-Chloro-10,11-dihydro-N,N-dimethyl-5H-dibenz[b,f]azepine-5-propanamine
Additional Names: 3-chloro-5-[3-(dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine; 5-(g-dimethylaminop...
Literature References: Serotonin reuptake inhibitor. Prepn: P. N. Craig et al., J. Org. Chem. 26, 135 (1961); W. Schindler, H. Dietrich, CH 371799; eidem, US 3467650 (1963, 1969 both to Geigy). Crystal and molecular structure of the hydrochloride: M. L. Post, A. S. Horn, Acta Crystallogr. 33B, 2590 (1977). HPLC determn in serum: H. Weigmann et al., J. Chromatogr. B 710, 227 (1998). Veterinary trial in canine compulsive disorder: C. J. Hewson et al., J. Am. Vet. Med. Assoc. 213, 1760 (1998); in canine separation anxiety: S. Petit et al., Rev. Med. Vet. 150, 133 (1999). Review of pharmacology and clinical experience in obsessive-compulsive disorder and depression: M. D. Peters et al., Clin. Pharm. 9, 165-178 (1990).

Femoxetine CAS Registry Number: 59859-58-4 非莫西汀

CAS Name: (3R,4S)-3-[(4-Methoxyphenoxy)methyl]-1-methyl-4-phenylpiperidine
Additional Names: (+)-trans-1-methyl-3-[p-(methoxy)phenoxymethyl]-4-phenylpiperidine
Percent Composition: C 77.14%,...
Literature References: Serotonin uptake inhibitor. Prepn: J. A. Christensen, R. F. Squires, BE 810310; eidem, US 3912743 (1974, 1975 both to A/S Ferrosan). Neuropharmacology: J. B. Lassen et al., Psychopharmacologia 42, 21 (1975). Pharmacology and toxicity: eidem, Eur. J. Pharmacol. 32, 108 (1975). GC determn in body fluids: E. Bechgaard, J. Lund, J. Chromatogr. 133, 147 (1977). Metabolism: H. Larsson, J. Lund, Acta Pharmacol. Toxicol. 48, 424 (1981). Bioavailability and pharmacokinetics: H. Mengel et al., Arzneim.-Forsch. 33, 462 (1983). Double-blind clinical trials in treatment of migraine: P. G. Andersson, E. N. Petersen, Acta Neurol. Scand. 64, 280 (1981); in treatment of endogenous depression: L.-E. Dahl et al., Acta Psychiatr. Scand. 66, 9 (1982); P. N. Reebye et al., Pharmacopsychiatria 15, 164 (1982).

Indeloxazine Hydrochloride CAS Registry Number: 65043-22-3 盐酸茚洛秦

CAS Name: 2-[(1H-Inden-7-yloxy)methyl]morpholine hydrochloride
Additional Names: (±)-2-[(7-indenyloxy)methyl]morpholine hydrochlorideTrademarks: Elen (Yamanouchi); Noin (Schering)
Perce...
Literature References: Serotonin uptake inhibitor. Prepn: M. Masuo et al., DE 2601703; eidem, US 4109088 (1976, 1978 both to Yamanouchi). Synthesis and resolution of isomers: T. Kojima et al., Chem. Pharm. Bull. 33, 3766 (1985). Pharmacology and toxicity: S. Tachikawa et al., Arch. Int. Pharmacodyn. 238, 81 (1979). Inhibition of synaptosomal uptake of serotonin and noradrenaline: M. Harada, H. Maeno, Biochem. Pharmacol. 28, 2645 (1979). GLC determn in human plasma: A. G. Hayes, T. Chang, J. Chromatogr. 272, 176 (1983).

Gemfibrozil CAS Registry Number: 25812-30-0 吉非罗齐

CAS Name: 5-(2,5-Dimethylphenoxy)-2,2-dimethylpentanoic acid
Additional Names: 2,2-dimethyl-5-(2,5-xylyloxy)valeric acidTrademarks: Decrelip (Ferrer); Genlip (Teofarma); Gevilon (Pfizer); Lipoz...
Literature References: Serum lipid regulating agent. Prepn: P. L. Creger, DE 1925423; eidem, US 3674836 (1969, 1972, both to Parke, Davis). Production: O. P. Goel, US 4126637 (1978 to Warner-Lambert). Pharmacology: A. H. Kissebach et al., Atherosclerosis 24, 199 (1976); M. T. Kahonen et al., ibid. 32, 47 (1979). Series of articles on metabolism, clinical pharmacology, kinetics and toxicology: Proc. R. Soc. Med. 69, Suppl 2, 1-120 (1976). Toxicity data: S. M. Kurtz et al., ibid. 15. Clinical trial in hyperlipidemia: J. E. Lewis et al., Pract. Cardiol. 9, 99 (1983). Clinical reduction of cardiovascular risk in patients with low HDL levels: H. B. Rubins et al., N. Engl. J. Med. 341, 410 (1999).

Bilobalide CAS Registry Number: 33570-04-6 (-)-白果内酯

CAS Name: (3aS,5aR,8R,8aS,9R,10aS)-9-(1,1-Dimethylethyl)-10,10a-dihydro-8,9-dihydroxy-4H,5aH,9H-furo[2,3-b]furo[3',2':2,3]cyclopenta[1,2-c]furan-2,4,7(3H,8H)trione
Percent Composition: C 55.21%...
Literature References: Sesquiterpene isolated from the leaves of Ginko biloba L., Ginkgoaceae; closely related to the ginkgolides, q.v. Component of the Ginkgo biloba extract, EGb 761, q.v. Isoln: K. Weinges, W. Bähr, Ann. 724, 214 (1969). NMR and MS analysis: eidem, ibid. 759, 158 (1972). Structure determn: K. Nakanishi et al., J. Am. Chem. Soc. 93, 3544 (1971). Total synthesis of (±)-form: E. J. Corey, W. Su, ibid. 109, 7534 (1987). Enantioselective synthesis of (-)-form: eidem, Tetrahedron Lett. 29, 3423 (1988). Separation from Ginkgo biloba extracts: S. Jaracz et al., Phytochemistry 65, 2897 (2004). Neuroprotective effects in animal models of brain ischemia: K. Chandrasekaran et al., Brain Res. 922, 282 (2001). GABAA antagonist activity: S. H. Huang et al., Eur. J. Pharmacol. 464, 1 (2003). Review of neuroprotective properties: F. V. Defeudis, Pharmacol. Res. 46, 565-568 (2002); of physical properties: T. A. van Beek, Bioorg. Med. Chem. 13, 5001-5012 (2005).

Parthenolide CAS Registry Number: 20554-84-1 小白菊内酯

CAS Name: (1aR,4E,7aS,10aS,10bS)-2,3,6,7,7a,8,10a,10b-Octahydro-1a,5-dimethyl-8-methyleneoxireno[9,10]cyclodeca[1,2-b]furan-9(1aH)-one
Additional Names: 4,5a-epoxy-6b-hydroxy-germacra-1(10),11(...
Literature References: Sesquiterpene lactone found in feverfew, q.v., and in other plants. Isolation from Chrysanthemum parthenium (L.) Bernh. Compositae and characterization: V. Herout et al., Chem. Ind. (London) 1959, 1069; M. Soucek et al., Collect. Czech. Chem. Commun. 26, 803 (1961); from Magnolia grandiflora L., Magnoliaceae: F. S. El-Feraly, Y.-M. Chan, J. Pharm. Sci. 67, 347 (1978). Revised structure and spectral analysis: T. R. Govindachari et al., Tetrahedron 21, 1509 (1965). Absolute configuration: A. S. Bawdekar et al., Tetrahedron Lett. 1966, 1225. Crystal structure: A. Quick, D. Rogers, J. Chem. Soc. Perkin Trans. 2 4, 465 (1976). HPLC determn: D. Strack et al., Z. Naturforsch. 35, 915 (1980). Cytotoxicity: K.-H. Lee et al., Cancer Res. 31, 1649 (1971); L. A. J. O'Neill et al., Br. J. Clin. Pharmacol. 23, 81 (1987).