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

Talipexole CAS Registry Number: 101626-70-4 他利克索

CAS Name: 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepin-2-amine
Additional Names: 6-allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine
Percent Composition: C 57.38%, H 7...
Literature References: a2-Adrenoceptor and dopamine D2-receptor agonist. Prepn: G. Griss et al., DE 2040510 (1972 to Thomae); eidem, US 3804849 (1974 to Boehringer, Ing.). Dopaminergic effects: P. A. Johansen et al., Life Sci. 43, 515 (1988); S. K. Kulkarni, K. Chopra, Methods Find. Exp. Clin. Pharmacol. 12, 99 (1990). Clinical evaluation in Parkinson's disease: Y. Mizuno et al., Drug Invest. 5, 186 (1993).

Mephentermine CAS Registry Number: 100-92-5 美芬丁胺

CAS Name: N,a,a-Trimethylbenzeneethanamine
Additional Names: 2-methylamino-2-methyl-1-phenylpropane; N-methyl-w-phenyl-tert-butylamine; N,a,a-trimethylphenethylamine
Percent Composition: C 8...
Literature References: a-Adrenergic agonist. Prepd by hydrogenating 1-chloro-2-methylamino-2-methyl-1-phenylpropane hydrochloride in methanol in the presence of palladium barium carbonate: Bruce, Szabo, US 2597445 (1952 to Wyeth). Alternate process: Abel et al., US 2590079 (1952 to Wyeth). Pharmacology: D. K. Eckfeld et al., J. Am. Pharm. Assoc. 43, 705 (1954).

Naphazoline CAS Registry Number: 835-31-4 萘甲唑啉

CAS Name: 4,5-Dihydro-2-(1-naphthalenylmethyl)-1H-imidazole
Additional Names: 2-(1-naphthylmethyl)imidazoline
Percent Composition: C 79.97%, H 6.71%, N 13.32%
Literature References: a-Adrenergic agonist. Prepd by reacting the acetic acid anhydride of naphthoimidic acid with ethylenediamine: A. Sonn, US 2161938 (1939 to Soc. Chem. Ind. Basle); by reacting naphthylthioacetamide with ethylenediamine: DK 62889 (1944 to Lovens Kemiske), C.A. 40, 4398 (1946). Toxicity data: J. Gylfe et al., Fed. Proc. 9, 280 (1950). Comprehensive description: G. M. Wall, Anal. Profiles Drug Subs. Excip. 21, 307-344 (1992).

Pholedrine CAS Registry Number: 370-14-9 甲羟苯丙胺

CAS Name: 4-[2-(Methylamino)propyl]phenol
Additional Names: p-hydroxy-N,a-dimethylphenethylamine; b-(p-hydroxyphenyl)isopropylmethylamine; a-(p-hydroxyphenyl)-b-methylaminopropane; p-hydroxy-N-...
Literature References: a-Adrenergic agonist. Prepd from p-methoxybenzyl methyl ketone: FR 822422, GB 482414, DE 674753 (1937, 1938 and 1939 to Knoll); Hildebrandt and Hildebrandt, Freese, DE 665793 and DE 767161 (1938 and 1951 to Knoll). Synthesis: Savitskii, Makhnenko, J. Gen. Chem. USSR 10, 1819 (1940); Buzas, Dufour, Bull. Soc. Chim. Fr. 1950, 139. Toxicity data: Lindner, Arch. Exp. Pathol. Pharmakol. 188, 675 (1938).

Octodrine CAS Registry Number: 543-82-8 1,5-二甲基己胺

CAS Name: 6-Methyl-2-heptanamine
Additional Names: 6-methyl-2-heptylamine; 2-methyl-6-aminoheptane; 6-amino-2-methylheptane; 2-amino-6-methylheptane; a,e-dimethylhexylamine; 1,5-dimethylhexylam...
Literature References: a-Adrenergic agonist. Prepd from the corresponding saturated ketone: Rohrmann, Shonle, J. Am. Chem. Soc. 66, 1516 (1944). Pharmacology: E. J. Fellows, J. Pharmacol. Exp. Ther. 90, 351 (1947).

Adrafinil CAS Registry Number: 63547-13-7 艾捉非尼

CAS Name: 2-[(Diphenylmethyl)sulfinyl]-N-hydroxyacetamide
Additional Names: 2-(benzhydrylsulfinyl)acetohydroxamic acidTrademarks: Olmifon (Lafon)
Percent Composition: C 62.26%, H 5.23%, N 4....
Literature References: a-Adrenergic agonist. Prepn, pharmacology: L. Lafon, BE 846880; US 4066686 (1977, 1978 both to Lafon). Mode of action: J. Duteil et al., Eur. J. Pharmacol. 59, 121 (1979); C. Rozé et al., Arch. Int. Pharmacodyn. Ther. 265, 119 (1983). Psychopharmacology in mice: F. A. Rambert et al., J. Pharmacol. 17, 37 (1986).

Nordefrin CAS Registry Number: 6539-57-7 (unspecified stereo); 74812-63-8 (R,S-(±)-form)

CAS Name: 4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol
Additional Names: a-(1-aminoethyl)-3,4-dihydroxybenzyl alcohol; 3,4-dihydroxynorephedrine; 3,4-dihydroxyphenylpropanolamine; 3,4-dihydroxyp...
Literature References: a-Adrenergic agonist. Prepn: DE 254438 (1912 to Bayer); W. H. Hartung et al., J. Am. Chem. Soc. 53, 4149 (1931); M. Bockmühl et al., US 1948162 (1934 to Winthrop); Bruckner et al., Ber. 76B, 466 (1943). Configuration: Fodor et al., Monatsh. Chem. 83, 1146 (1952). Prepn of optical isomers: DE 269327 (1913 to Bayer); Bockmühl, Gorr, DE 639126 (1936 to I. G. Farbenind.). Pharmacology: F. P. Luduena et al., J. Dent. Res. 37, 206 (1958). HPLC determn in plasma: D. A. Jenner et al., J. Chromatogr. 224, 507 (1981). Effect on toxicity of local anesthetics: S. E. Taylor, R. L. Dorris, Anesth. Prog. 36, 79 (1989). Review of use in local anesthesia: T. M. Hensley et al., J. Foot Surg. 26, 504-510 (1987).

Metizoline CAS Registry Number: 17692-22-7 美替唑啉

CAS Name: 4,5-Dihydro-2-[(2-methylbenzo[b]thien-3-yl)methyl]-1H-imidazole
Additional Names: 2-[(2-methylbenzo[b]thien-3-yl)methyl]-2-imidazoline; 2-methyl-3-(D2-imidazolinylmethyl)benzo[b]thiop...
Literature References: a-Adrenergic agonist. Prepn: FR M1614; FR 1355049 (1963, 1964 both to E. Merck), C.A. 58, 12574e (1963); 61, 4146e (1964). Pharmacology and toxicity: G. F. Rosati, M. G. Poletto, Farmaco Ed. Prat. 21, 204 (1966).

Tramazoline CAS Registry Number: 1082-57-1 曲马唑啉

CAS Name: 4,5-Dihydro-N-(5,6,7,8-tetrahydro-1-naphthalenyl)-1H-imidazol-2-amine
Additional Names: 2-[(5,6,7,8-tetrahydro-1-naphthyl)amino]-2-imidazoline
Percent Composition: C 72.53%, H 7.96...
Literature References: a-Adrenergic agonist. Prepn: Berg, DE 1191381; DE 1195323 (both 1965 to Thomae), C.A. 63, 8373c; 13274d (1965). Pharmacology and toxicity data: R. Engelhorn, H. Klupp, Arzneim.-Forsch. 12, 971 (1962). Activity studies: Sachsenröder et al., ibid. 22, 392 (1972).

Phenylephrine CAS Registry Number: 59-42-7 去氧肾上腺素

CAS Name: (aR)-3-Hydroxy-a-[(methylamino)methyl]benzenemethanol
Additional Names: (-)-m-hydroxy-a-[(methylamino)methyl]benzyl alcohol; l-1-(m-hydroxyphenyl)-2-methylaminoethanol; l-a-hydroxy-b-...
Literature References: a-Adrenergic agonist. Prepn: H. Legerlotz, US 1932347 (1933 to Frederick Stearns); E. D. Bergmann, M. Sulzbacher, J. Org. Chem. 16, 84 (1951); M. K. Gurjar et al., Org. Process Res. Dev. 2, 422 (1998). Spectrophotometric determn: S. A. Shama, J. Pharm. Biomed. Anal. 30, 1385 (2002). Toxicity data: M. R. Warren, H. W. Werner, J. Pharmacol. Exp. Ther. 86, 284 (1946). Clinical efficacy in mydriasis: V. Tanner, A. G. Casswell, Eye 10, 95 (1996). Clinical evaluation in fecal incontinence: M. J. Cheetham et al., Gut 48, 356 (2001). Comprehensive description: C. A. Gaglia, Jr., Anal. Profiles Drug Subs. 3, 483-512 (1974). Review of ophthalmologic uses: S. M. Meyer, F. T. Fraunfelder, Ophthalmology 87, 1177-1180 (1980); of clinical trials vs ephedrine, q.v., in treatment of hypotension during cesarean delivery: A. Lee et al., Anesth. Analg. 94, 920-926 (2002).