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

Amidephrine CAS Registry Number: 3354-67-4

CAS Name: N-[3-[1-Hydroxy-2-(methylamino)ethyl]phenyl]methanesulfonamide
Additional Names: 3'-[1-hydroxy-2-(methylamino)ethyl]methanesulfonanilidePercent Composition: C 49.16%, H 6.60%, N 11.47...
Literature References: a1 Adrenoceptor agonist. Prepn: Larsen, Uloth, FR M3027 (1965 to Mead Johnson), C.A. 62, 13091a (1965); Uloth et al., J. Med. Chem. 9, 88 (1966). Pharmacology of the racemate: Dungan et al., Int. J. Neuropharmacol. 4, 219 (1965); Stanton et al., ibid. 235; of the isomers: Larsen, Lish, Nature 203, 1283 (1964); Buchthal, Jenkinson, Eur. J. Pharmacol. 10, 293 (1970). Toxicology: J. H. Weikel, Jr., K. H. Harper, Toxicol. Appl. Pharmacol. 23, 589 (1972).

Silodosin CAS Registry Number: 160970-54-7 西洛多辛

CAS Name: 2,3-Dihydro-1-(3-hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-1H-indole-7-carboxamidePercent Composition: C 60.60%, H 6.51%, F 11.50%, N 8.48%, O 12...
Literature References: a1a-Adrenoceptor antagonist. Prepn: M. Kitazawa et al., EP 600675; eidem, US 5387603 (1994, 1995 both to Kissei). Adrenoceptor binding study: K. Shibata et al., Mol. Pharmacol. 48, 250 (1995); and tissue selectivity: S. Murata et al., J. Urol. 164, 578 (2000). Pharmacology: K. Akiyama et al., Pharmacology 64, 140 (2002). Series of articles on pharmacology, pharmacokinetcs and toxicology: Yakugaku Zasshi 126, 187-263 (2006). Review of development and therapeutic potential: F. Kamali, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 1, 248-252 (1999).

Urapidil CAS Registry Number: 34661-75-1 乌拉地尔

CAS Name: 6-[[3-[4-(2-Methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione
Additional Names: 6-[[3-[4-(o-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethylura...
Literature References: a1-Adrenergic antagonist; deriv of uracil, q.v. Prepn: W. Pruesse et al., DE 1942405; eidem, US 3957786 (1971, 1976 both to Byk Gulden); K. Klemm et al., Arzneim.-Forsch. 27, 1895 (1977). Series of articles on pharmacology, pharmacokinetics, metabolism: ibid. 1898-1932. Toxicity data: J. Koenig et al., ibid. 1919. Mode of action: M. Eltze, Eur. J. Pharmacol. 59, 1 (1979); H. R. Kaplan, R. D. Smith, Fed. Proc. 40, 2268 (1981). Hemodynamic responses in man: G. G. Belz et al., Clin. Pharmacol. Ther. 37, 48 (1985). Clinical trials: A. Barankay et al., Arzneim.-Forsch. 31, 849 (1981); H. Liebau et al., J. Hypertens. 4, Suppl. 6, S141 (1986). Series of articles on clinical efficacy in hypertension: Drugs 35, Suppl. 6, 147-192 (1988).

Naftopidil CAS Registry Number: 57149-07-2 萘哌地尔

CAS Name: 4-(2-Methoxyphenyl)-a-[(1-naphthalenyloxy)methyl]-1-piperazineethanol
Additional Names: RS-1-[4-(2-methoxyphenyl)-1-piperazinyl]-3-(1-naphthoxy)-2-propanol; 1-(2-methoxyphenyl)-4-[3-(...
Literature References: a1-Adrenergic blocker and serotonin (5HT1A) receptor agonist. Prepn: E. C. Witte et al., DE 2408804; eidem, US 3997666 (1975, 1976 both to Boehringer Mann.). Clinical pharmacodynamics: R. Kirsten et al., Eur. J. Clin. Pharmacol. 46, 271 (1994). Clinical pharmacokinetics: M. J. G. Farthing et al., Postgrad. Med. J. 70, 363 (1994). HPLC determn in human plasma: G. Niebch et al., J. Chromatogr. 534, 247 (1990). Clinical evaluation in BPH: K. Yasuda et al., Prostate 25, 46 (1994). Review of pharmacology and clinical experience: H. M. Himmel, Cardiovasc. Drug Rev. 12, 32-47 (1994).

Raubasine CAS Registry Number: 483-04-5 萝巴新; 阿吗碱

CAS Name: (19a)-16,17-Didehydro-19-methyloxayohimban-16-carboxylic acid methyl ester
Additional Names: d-yohimbine; pytetrahydroserpentine; tetrahydroserpentine; ajmalicine
Trademarks: Circo...
Literature References: a1-Adrenergic blocker isolated from bark of Corynanthe johimbe K. Schum., Rubiaceae: H. Heinemann, Ber. 67, 15 (1934); from roots of Rauwolfia serpentina (L.) Benth., Apocynaceae: S. Siddiqui, R. H. Siddiqui, J. Indian Chem. Soc. 8, 667 (1931); A. H. Popelak et al., Naturwissenschaften 40, 625 (1953); A. Hofmann, Helv. Chim. Acta 37, 849 (1954); M. W. Klohs et al., J. Am. Chem. Soc. 76, 1332 (1954). Review of early literature: R. E. Woodson et al., Rauwolfia: Botany, Pharmacognosy, Chemistry and Pharmacology (Little, Brown and Co., Boston, 1957) 147 pp. Structure: Goutarel, Le Hir, Bull. Soc. Chim. Fr. 18, 909 (1951). Stereochemistry: Wenkert et al., J. Am. Chem. Soc. 83, 5037 (1961); Shamma, Richey, ibid. 85, 2507 (1963). Total synthesis of dl-form: van Tamelen, Placeway, ibid. 83, 2594 (1961); van Tamelen et al., ibid. 91, 7359 (1969); J. Gutzwiller et al., Helv. Chim. Acta 64, 1663 (1981); T. Kametani et al., J. Chem. Soc. Perkin Trans. 1 1981, 3168. Biosynthesis: N. Nagakura et al., ibid. 1979, 2308; M. Rueffer et al., Chem. Commun. 1979, 1016. Pharmacokinetics: A. Marzo et al., Farmaco Ed. Prat. 36, 173 (1981). Clinical evaluation of platelet anti-aggregant activity: J. Neuman et al., Arzneim.-Forsch. 36, 1394 (1986). Evaluation of combination with almitrine, q.v., in cerebral ischemia in rats: M. G. Borzeix, J. Cahn, ibid. 37, 491 (1987).

Terazosin CAS Registry Number: 63590-64-7 特拉唑嗪

CAS Name: 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetrahydro-2-furanyl)carbonyl]piperazine
Additional Names: 2-[(4-tetrahydro-2-furoyl)-1-piperazinyl]-4-amino-6,7-dimethoxyquinazoline
P...
Literature References: a1-Adrenergic blocker related to prazosin, q.v. Prepn: M. Winn et al., DE 2646186; eidem, US 4026894 (both 1977 to Abbott); of the hydrochloride dihydrate: R. Roteman, DE 2831112; idem, US 4251532 (1979, 1981 both to Abbott). HPLC determn in biological fluids: S. E. Patterson, J. Chromatogr. 311, 206 (1984). Toxicity in rats: F. L. Fort et al., Drug Chem. Toxicol. 7, 435 (1984). Clinical study in essential hypertension: P. A. Abraham et al., Pharmacotherapy 5, 285 (1985); in treatment of benign prostatic hyperplasia: H. Lepor et al., J. Urol. 148, 1467 (1992). Symposium on pharmacology, pharmacokinetics, and clinical efficacy in hypertension: Am. J. Med. 80, Suppl. 5B, 1-105 (1986). Comprehensive description: Z. L. Chang, J. F. Bauer, Anal. Profiles Drug Subs. 20, 693-727 (1991). Review of pharmacology and therapeutic efficacy: R. Achari, A. Laddu, J. Clin. Pharmacol. 32, 520-523 (1992).

Moxisylyte CAS Registry Number: 54-32-0 莫西赛利

CAS Name: 4-[2-(Dimethylamino)ethoxy]-2-methyl-5-(1-methylethyl)phenol acetate (ester)
Additional Names: 5-(2-dimethylaminoethoxy)carvacrol acetate; 6-acetoxythymol 2-(dimethylamino)ethyl ether...
Literature References: a1-Adrenergic blocker. Prepn: H. Pahlicke, DE 905738 (1954 to Diwag), C.A. 52, 16294i (1958); A. Buzas et al., Bull. Soc. Chim. Fr. 1959, 839. Pharmacology: K. Greeff, H. J. Schümann, Arzneim.-Forsch. 3, 341 (1953); J. Mercier et al., Therapie 26, 785 (1971). Toxicology: J. Roquebert, J. Canellas, ibid. 775. a-Adrenergic antagonist activity: A. T. Birmingham, J. Szolcsanyi, J. Pharm. Pharmacol. 17, 449 (1965). a1-receptor selectivity: J. Roquebert et al., Arch. Int. Pharmacodyn. 266, 282 (1983). Series of articles on metabolism: K.-O. Vollmer et al., Eur. J. Drug Metab. Pharmacokinet. 10, 61, 71, 139 (1985). Clinical pharmacokinetics: P. Costa et al., J. Pharm. Sci. 82, 729, 968 (1993). HPLC determn of metabolites in plasma and urine: C. Marquer, F. Bressolle, J. Chromatogr. B 691, 389 (1997). Clinical trial in Raynaud's disease and chilblains: G. V. Jaffe, J. J. Grimshaw, Br. J. Clin. Pract. 34, 343 (1980). Review of clinical studies in ophthalmology: M. Wand, W. M. Grant, Surv. Ophthalmol. 25, 75-84 (1980). Clinical trial in impotence: P. Costa et al., J. Urol. 149, 301 (1993).

Alfuzosin CAS Registry Number: 81403-80-7 阿夫唑嗪

CAS Name: N-[3-[(4-Amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furancarboxamide
Additional Names: N1-(4-amino-6,7-dimethoxyquinazol-2-yl)-N1-methyl-N2-(tetrahydrofuroyl-2...
Literature References: a1-Adrenoceptor antagonist structurally similar to prazosin, q.v. Prepn: P. M. J. Manoury, DE 2904445; idem, US 4315007 (1979, 1982 both to Synthelabo); and antihypertensive activity in rats: P. M. Manoury et al., J. Med. Chem. 29, 19 (1986). Pharmacology: A. G. Ramage, Eur. J. Pharmacol. 129, 307 (1986). HPLC determn in biological fluids: P. Guinebault et al., J. Chromatogr. 353, 361 (1986). Pharmacology in humans: A. H. Deering, Br. J. Clin. Pharmacol. 25, 417 (1988). Clinical evaluation in essential hypertension: S. Leto Di Priolo et al., Eur. J. Clin. Pharmacol. 35, 25 (1988); A. K. Ghosh, S. Ghosh, Ger. Cardiovasc. Med. 1, 81 (1988). Clinical trial in benign prostatic hyperplasia (BPH): C. G. Roehrborn et al., BJU Int. 92, 257 (2003). Review of clinical experience in BPH: D. M. Weiner, F. C. Lowe, Expert Opin. Pharmacother. 4, 2057-2063 (2003).

Binodenoson CAS Registry Number: 144348-08-3 2-(环己基亚甲基肼基)腺苷酸

CAS Name: 2-[(Cyclohexylmethylene)hydrazino]adenosinePercent Composition: C 52.16%, H 6.44%, N 25.05%, O 16.35%
Literature References: A2A-adenosine receptor agonist, more selective than adenosine, q.v. Prepn: R. A. Olsson, R. D. Thompson, EP 567094; eidem, US 5278150 (1993, 1994 both to Whitby Research); K. Niiya et al., J. Med. Chem. 35, 4557 (1992). Dose ranging and clinical evaluation as coronary vasodilator in myocardial imaging: J. E. Udelson et al., Circulation 109, 457 (2004). Clinical pharmacokinetics: R. J. Barrett et al., J. Nucl. Cardiol. 12, 166 (2005). Review: A. Zaza, Curr. Opin. Cardiovasc. Pulm. Renal Invest. Drugs 1, 301-306 (1999).

Mivazerol CAS Registry Number: 125472-02-8 米伐折醇

CAS Name: 2-Hydroxy-3-(1H-imidazol-4-ylmethyl)benzamide
Additional Names: a-imidazol-4-yl-2,3-cresotamide
Percent Composition: C 60.82%, H 5.10%, N 19.34%, O 14.73%
Literature References: a2-Adrenergic agonist. Prepn: E. Cossement et al., EP 341231; eidem, US 4923865 (1989, 1990 both to UCB); idem et al., J. Pharm. Belg. 49, 206 (1994). Specificity for a2 adrenoceptors and binding studies: M. Noyer et al., Neurochem. Int. 24, 221 (1994). Clinical trial to improve perioperative hemodynamic stability: D. T. Mangano et al., Anesthesiology 86, 346 (1997). Mode of action study: M. Guyaux et al., Acta Anaesthesiol. Scand. 42, 238 (1998).