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

Dexmedetomidine CAS Registry Number: 113775-47-6 右美托嘧啶

CAS Name: 4-[(1S)-1-(2,3-Dimethylphenyl)ethyl]-1H-imidazole
Additional Names: d-medetomidinePercent Composition: C 77.96%, H 8.05%, N 13.99%
Literature References: a2-Adrenergic agonist; (+)-isomer of medetomidine, q.v. Prepn: A. J. Karjalainen et al., GB 2206880; eidem, US 4910214 (1989, 1990 both to Farmos). Physical properties: R. Rajala et al., Eur. J. Pharm. Sci. 1, 219 (1994). Clinical pharmacokinetics: P. Talke et al, Anesth. Analg. 85, 1136 (1997). Clinical evaluation as anesthetic adjunct: J. Jalonen et al., Anesthesiology 86, 331 (1997). Review of pharmacology and clinical experience for sedation of patients in intensive care: N. Bhana et al., Drugs 59, 263-270 (2000).

Tizanidine CAS Registry Number: 51322-75-9 替扎尼定

CAS Name: 5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
Additional Names: 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole
Percent Composition: C 42.61%, ...
Literature References: a2-Adrenergic agonist; centrally active myotonolytic. Prepn and antitremor activity: P. Neumann, NL 7306228; eidem, US 3843668 (1973, 1974 both to Wander-Sandoz). Pharmacology: A. C. Sayers et al., Arzneim.-Forsch. 30, 793 (1980); and mechanism of action studies: L. Turski et al., Brain Res. 379, 367 (1986); H. Ono et al., Gen. Pharmacol. 17, 137 (1986). Pharmacokinetics: V. Heazlewood et al., Eur. J. Clin. Pharmacol. 25, 65 (1983). Clinical evaluation in spasticity of multiple sclerosis: P. M. Newman et al., ibid. 23, 31 (1982); M. C. Hoogstraten et al., Acta Neurol. Scand. 77, 224 (1988).

Apraclonidine CAS Registry Number: 66711-21-5 阿可乐定

CAS Name: 2,6-Dichloro-N1-(4,5-dihydro-1H-imidazol-2-yl)-1,4-benzenediamine
Additional Names: 2,6-dichloro-N'-2-imidazolidinylidene-1,4-benzenediamine; 2-[(4-amino-2,6-dichlorophenyl)imino]imid...
Literature References: a2-Adrenergic agonist; structural analog of clonidine, q.v. Synthesis: B. Rouot, G. LeClerc, Bull. Soc. Chim. Fr. Pt. 2, 520 (1979). Prepn (not claimed) and use in treatment of intraocular pressure: B. M. York, Jr., US 4517199 (1985 to Alcon). Pharmacology: B. Rouot et al., C.R. Seances Acad. Sci. Ser. D 286, 909 (1978). Receptor binding studies: D. C. U'Prichard, Prog. Clin. Biol. Res. 71, 53 (1981). D. C. Stump, D. E. MacFarlane, J. Lab. Clin. Med. 102, 779 (1983). Clinical pharmacology: D. A. Abrams et al., Arch. Ophthalmol. 105, 1205 (1987). Clinical evaluation in treatment of intraocular pressure: A. L. Robin et al., ibid. 1208; as additive to maximally tolerated medical therapy in glaucoma: A. L. Robin et al., Am. J. Ophthalmol. 120, 423 (1995).

Idazoxan CAS Registry Number: 79944-58-4 亚达唑散

CAS Name: 2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole
Additional Names: 2-[2-(1,4-benzodioxanyl)]-2-imidazoline
Percent Composition: C 64.69%, H 5.92%, N 13.72%, O 15.67%
Literature References: a2-Adrenergic blocker. Prepn: J. Krapcho, W. A. Lott, US 2979511 (1961 to Olin Mathieson); and confirmation of structure: C. B. Chapleo, P. L. Myers, Tetrahedron Lett. 22, 4839 (1981). Structure-activity study: C. B. Chapleo et al., J. Med. Chem. 26, 823 (1983). Pharmacology: H. Dabiré, J. Pharmacol. 17, 113 (1986). Clinical evaluation in progressive supranuclear palsy: D. G. Cole, J. H. Growdon, J. Neural Transm. Suppl. 42, 283 (1994); as adjunct to fluphenazine in schizophrenia: R. E. Litman et al., Br. J. Psychiatry 168, 571 (1996).

Lofexidine CAS Registry Number: 31036-80-3 洛非西定

CAS Name: 2-[1-(2,6-Dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
Additional Names: 2-[1-(2,6-dichlorophenoxy)ethyl]-2-imidazoline
Percent Composition: C 50.99%, H 4.67%, Cl 27.36%, N 10.8...
Literature References: a2-Adrenoceptor agonist related structurally to clonidine, q.v. Prepn of the HCl salt: H. Baganz, H. J. May, ZA 6800850; eidem, US 3966757 (1968, 1976 both to Nordmark); of the free base: eidem, DE 1935479 (1971 to Nordmark), C.A. 74, 87979 (1971). Pharmacological studies: J. Velly, J. Pharmacol. 8, 351 (1977); B. Jarrot et al., Biochem. Pharmacol. 28, 141 (1979). NMR data and cardiovascular effects: P. B. M. Timmermans, P. A. Van Zwieten, Eur. J. Med. Chem. 15, 323 (1980). Hypotensive and sedative properties: P. Birch et al., Br. J. Pharmacol. 68, 107 (1980). Effects in hypertension: N. D. Vlachakis et al., Fed. Proc. 39, 4844 (1980). Series of articles on pharmacology, toxicology, clinical studies: Arzneim.-Forsch. 32, 915-993 (1982). Toxicity studies: T. H. Tsai et al., ibid. 955. Review of clinical trials in treatment of opiate withdrawal: J. Strang et al., Am. J. Addict. 8, 337-348 (1999).

Detomidine CAS Registry Number: 76631-46-4 地托咪定

CAS Name: 4-[(2,3-Dimethylphenyl)methyl]-1H-imidazole
Additional Names: 4-(2',3'-dimethylbenzyl)imidazole
Percent Composition: C 77.38%, H 7.58%, N 15.04%
Literature References: a2-Adrenoceptor agonist with sedative and analgesic activity. Prepn: A. J. Karjalayne, K. O. A. Kurkela, EP 24829; eidem, US 4443466 (1981, 1984 both to Farmos). Physical studies: E. Laine et al., Acta Pharm. Suec. 20, 451 (1983). Crystal structure: L. H. J. Lajunen et al., ibid. 21, 163 (1984). Pharmacology: R. Virtanen, L. Nyman, Eur. J. Pharmacol. 108, 163 (1985); R. Virtanen, E. MacDonald, ibid. 115, 277 (1985). Mechanism of action: eidem, J. Vet. Pharmacol. Ther. 8, 30 (1985).

Moxonidine CAS Registry Number: 75438-57-2 莫索尼定

CAS Name: 4-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamine
Additional Names: 4-chloro-6-methoxy-2-methyl-5-(2-imidazolin-2-yl)aminopyrimidineTrademarks: Cynt (Beier...
Literature References: a2-Adrenoceptor agonist. Prepn: NL 7908192; W. Stenzel et al., US 4323570 (1980, 1982 both to Beiersdorf AG). Series of articles on pharmacology and binding studies: Arzneim.-Forsch. 38, 1426-1445 (1988). Pharmacokinetics: D. Trenk et al., J. Clin. Pharmacol. 27, 988 (1987); W. Kirch et al., ibid. 30, 1088 (1990). Clinical comparison with clonidine, q.v.: V. Plänitz, ibid. 27, 46 (1987).

Rilmenidine CAS Registry Number: 54187-04-1 利美尼啶

CAS Name: N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine
Additional Names: 2-[N-(dicyclopropylmethyl)amino]oxazoline; oxaminozolinePercent Composition: C 66.63%, H 8.95%, N 15.54%, O 8.88%
Literature References: a2-Adrenoceptor agonist. Prepn: C. Malen et al., DE 2362754; eidem, US 4102890 (1974, 1978 both to Sci. Union et Cie. - Soc. Franc. Recher. Med.). Adrenoceptor binding study: P. Guicheney et al., J. Pharmacol. 12, 255 (1981). Pharmacokinetics in hypertensive subjects: J. Velly et al., ibid. 13, 413 (1982). Animal pharmacology: M. Laubie et al., ibid. 16, 259 (1985); P. A. van Zwieten et al., Arch. Int. Pharmacodyn. 279, 130 (1986). Hypotensive effect in humans: K. Weerasuriya et al., Eur. J. Clin. Pharmacol. 27, 281 (1984). Mechanism of action study: R. E. Gomez et al., Eur. J. Pharmacol. 195, 181 (1991). Review: T. J. Verbeuren et al., Cardiovasc. Drug Rev. 8, 56-70 (1990).

Brimonidine CAS Registry Number: 59803-98-4 溴莫尼定

CAS Name: 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine
Additional Names: 5-bromo-6-(2-imidazolin-2-ylamino)quinoxalinePercent Composition: C 45.23%, H 3.45%, Br 27.35%, N 23.97%
Literature References: a2-Adrenoceptor agonist. Prepn: J. C. Danielewicz et al., DE 2309160; eidem, US 3890319 (1973, 1975 both to Pfizer). HPLC determn in serum and aqueous humour of the eye: N. K. Karamanos et al., Biomed. Chromatogr. 13, 86 (1999). Clinical study in control of intraocular pressure: R. David et al., Arch. Ophthalmol. 111, 1387 (1993); L. J. Katz et al., Am. J. Ophthalmol. 127, 20 (1999). Review of pharmacology and mechanisms of action: J. C. Adkins, J. A. Balfour, Drugs Aging 12, 225-241 (1998); of pharmacotherapeutic profile: L. B. Cantor, Expert Opin. Pharmacother. 1, 815-834 (2000).

Ecabapide CAS Registry Number: 104775-36-2 依卡派特

CAS Name: 3-[[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-2-oxoethyl]amino]-N-methylbenzamide
Additional Names: m-[[[(3,4-dimethoxyphenethyl)carbamoyl]methyl]amino]-N-methylbenzamide; ecabamidePerc...
Literature References: a2-Adrenoceptor agonist; reduces vagally-induced gastric acid secretion. Prepn: T. Miki et al., EP 185368; eidem, US 4985595 (1986, 1991 both to Daiichi); T. Hosokami et al., Chem. Pharm. Bull. 40, 2712 (1992). Pharmacology: K. Yokotani et al., Jpn. J. Pharmacol. 48, 299 (1988); M. Hirohashi et al., Arzneim.-Forsch. 43, 569 (1993). Efficacy in exptl ulcers: M Asano et al., ibid. 40, 276 (1990). Metabolism studies: Y. Fujimaki et al., Xenobiotica 25, 501 (1995).