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

Nialamide CAS Registry Number: 51-12-7 烟肼酰胺

CAS Name: 4-Pyridinecarboxylic acid 2-[3-oxo-3-[(phenylmethyl)amino]propyl]hydrazide
Additional Names: 1-[2-(benzylcarbamoyl)ethyl]-2-isonicotinoylhydrazide; N-[2-(benzylcarbamyl)ethylamino]iso...
Literature References: Monoamine oxidase (MAO) inhibitor. Prepn: Bloom, Carnahan, US 2894972; US 3040061 (1959, 1962 both to Pfizer). Toxicology study: C. S. Delahunt, J. M. Pepin, Toxicol. Appl. Pharmacol. 1, 524 (1959).

Octamoxin CAS Registry Number: 4684-87-1 奥他莫辛

CAS Name: (1-Methylheptyl)hydrazine
Additional Names: 2-hydrazinooctane; octomoxine
Trademarks: Ximaol
Percent Composition: C 66.61%, H 13.97%, N 19.42%
Literature References: Monoamine oxidase inhibitor. Prepd by condensation of methyl hexyl ketone and hydrazine hydrate followed by hydrogenation under pressure: Michel-Ber et al., GB 899385 (1962 to Soc. Civile Auguil).

Iproniazid CAS Registry Number: 54-92-2 N'-异丙基异烟肼

CAS Name: 4-Pyridinecarboxylic acid 2-(1-methylethyl)hydrazide
Additional Names: isonicotinic acid 2-isopropylhydrazide; 1-isonicotinoyl-2-isopropylhydrazine; 1-isonicotinyl-2-isopropylhydrazin...
Literature References: Monoamine oxidase inhibitor. Prepd by treating isoniazid with isopropyl bromide in abs alcohol in the presence of sodium: McMillan et al., J. Am. Pharm. Assoc. Sci. Ed. 42, 457 (1953). Alternate synthesis: Fox, Gibas, J. Org. Chem. 18, 994 (1953). Comprehensive description: F. Belal, H. Abdel-Aliem, Anal. Profiles Drug Subs. 20, 337-368 (1991).

Pargyline CAS Registry Number: 555-57-7 N-甲基-N-炔丙基苯甲胺

CAS Name: N-Methyl-N-2-propynylbenzenemethanamine
Additional Names: N-methyl-N-2-propynylbenzylamine; N-benzyl-N-methyl-2-propynylamine; N-methyl-N-propargylbenzylamineTrademarks: Eudatin (Abbo...
Literature References: Monoamine oxidase inhibitor. Prepd from propargyl bromide and benzylmethylamine: GB 906245; Martin, US 3155584 (1962 and 1964, both to Abbott). Activity as a glucuronyl transferase inducer: Yeh, Mitchell, Experientia 28, 298 (1972).

Tranylcypromine CAS Registry Number: 155-09-9 rel-(1R,2S)-2-苯基环丙烷-1-胺

CAS Name: (1R,2S)-rel-2-PhenylcyclopropanaminePercent Composition: C 81.16%, H 8.32%, N 10.52%
Literature References: Monoamine oxidase inhibitor. Prepn: Burger, Yost, J. Am. Chem. Soc. 70, 2198 (1948); R. E. Tedeschi, US 2997422 (1961 to SK F).

Isocarboxazid CAS Registry Number: 59-63-2 异卡波肼

CAS Name: 5-Methyl-3-isoxazolecarboxylic acid 2-benzylhydrazide
Additional Names: 3-(N-benzylhydrazinocarbonyl)-5-methylisoxazole; 1-benzyl-2-(5-methyl-3-isoxazolylcarbonyl)hydrazineTrademarks:...
Literature References: Monoamine oxidase inhibitor. Prepn: Gardner, Wenis, US 2908688 (1959 to Hoffmann-La Roche); J. Med. Pharm. Chem. 2, 133 (1960). Comprehensive description: B. C. Rudy, B. Z. Senkowski, Anal. Profiles Drug Subs. 2, 295-314 (1973).

Iproclozide CAS Registry Number: 3544-35-2 异丙氯肼

CAS Name: 4-(Chlorophenoxy)acetic acid 2-(1-methylethyl)hydrazide
Percent Composition: C 54.44%, H 6.23%, Cl 14.61%, N 11.54%, O 13.18%
Literature References: Monoamine oxidase inhibitor. Prepn: Libermann, Denis, Bull. Soc. Chim. Fr. 1961, 1952. GC determn in urine: R. M. DeSagher et al., Anal. Chem. 47, 1144 (1976).

Bifemelane CAS Registry Number: 90293-01-9 二苯美伦

CAS Name: N-Methyl-4-[2-(phenylmethyl)phenoxy]-1-butanamine
Additional Names: 4-(o-benzylphenoxy)-N-methylbutylamine; 2-(4-methylaminobutoxy)diphenylmethane; 2-benzyl-1-[4-(methylamino)butoxy]b...
Literature References: Monoamine oxidase inhibitor. Prepn: R. Kikumoto et al., DE 2627227; eidem, US 4091114 (1976, 1978 both to Mitsubishi); and antidepressant activity: R. Kikumoto et al., J. Med. Chem. 24, 145 (1981). Pharmacology: A. Tobe et al., Arzneim.-Forsch. 31, 1278 (1981). Effects on experimental amnesia in rats: A. Tobe et al., Jpn. J. Pharmacol. 39, 153 (1985). Effects on neuronal activity in cats: M. Egawa et al., Neuropharmacology 26, 379 (1987). Inhibition of MAO: M. Naoi et al., J. Neurochem. 50, 243 (1988).

Selegiline CAS Registry Number: 14611-51-9 司来吉兰盐酸盐

CAS Name: (aR)-N,a-Dimethyl-N-2-propynylbenzeneethanamine
Additional Names: L-(-)-N,a-dimethyl-N-2-propynylphenethylamine; (-)-deprenil; L-deprenyl
Percent Composition: C 83.37%, H 9.15%, N ...
Literature References: Monoamine oxidase-B inhibitor related structurally to pargyline, q.v. Prepn of racemate: FR M 2635 (1964 to Chinoin), C.A. 63, 2927e (1965); of (-)-form: NL 6605956 (1966 to Chinoin), C.A. 67, 21611y (1967); J. S. Fowler, J. Org. Chem. 42, 2637 (1977). See also: Z. Ecsery et al., US 4564706 (1986 to Chinoin). Effects of racemate on CNS: J. Knoll et al., Arch. Int. Pharmacodyn. 155, 154 (1965). Comparative pharmacology of isomers: K. Magyar et al., Acta Physiol. Acad. Sci. Hung. 32, 377 (1967). Preliminary study in Alzheimer's disease: L. S. Schneider et al., Am. J. Psychiatry 150, 321 (1993). Review of pharmacology: E. H. Heinonen, R. Lammintausta, Acta Neurol. Scand. 84, Suppl 136, 44-59 (1991); of efficacy in Parkinson's disease: D. W. Robin, Am. J. Med. Sci. 302, 392-395 (1991). Symposium: Mov. Disord. 8, Suppl. 1, S1-S44 (1993). Review of veterinary use in canine cognitive dysfunction: W. W. Ruehl, B. L. Hart in Psychopharmacology of Animal Behavior Disorders, N. H. Dodman, L. Shuster, Eds. (Blackwell Sci., Malden, Mass., 1998) pp 283-304.

Scopolin CAS Registry Number: 531-44-2 东莨菪甙; 东莨菪苷

CAS Name: 7-(b-D-Glucopyranosyloxy)-6-methoxy-2H-1-benzopyran-2-one
Percent Composition: C 54.24%, H 5.12%, O 40.64%
Literature References: Mono-b-glucopyranoside of scopoletin. From root of Scopolia japonica Maxim., S. carniolica Jacq., Solanaceae and Nerium odorum Sol., Apocynaceae. Isoln: Eykman, Ber. 17 III, 442 (1884); Ritter et al., Helv. Chim. Acta 36, 434 (1953). Synthesis: Merz, Arch. Pharm. 270, 476 (1932). Possible identity with murrayin: Bose, Mookerjee, J. Indian Chem. Soc. 14, 489 (1937). Chromatography, and spectrum of murrayin: Chakraborty, Bose, ibid. 33, 905 (1956); Chakraborty, Chakraborty, Trans. Bose Res. Inst. (Calcutta) 24 (1), 15 (1961), C.A. 55, 24228c (1961).