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

Sumatrol CAS Registry Number: 82-10-0 11-羟基鱼藤酮

CAS Name: [2R-(2a,6aa,12aa)]-1,2,12,12a-Tetrahydro-5-hydroxy-8,9-dimethoxy-2-(1-methylethenyl)-[1]benzopyrano[3,4-b]furo[2,3-h][1]benzopyran-6(6aH)-one
Percent Composition: C 67.31%, H 5.40%, O...
Literature References: Present in resin from Derris sp., Leguminosae: Robertson, Rusby, J. Chem. Soc. 1937, 497. Isolated also from Tephrosia toxicaria Pers., Papilionaceae: Harper, ibid. 1940, 1178. Structure and stereochemistry: Harper, loc. cit.; Crombie, Peace, ibid. 1961, 5445.

Pseudoyohimbine CAS Registry Number: 84-37-7 (3b)-17alpha-羟基育亨宾-16b-羧酸甲酯

CAS Name: (3b,16a,17a)-17-Hydroxyyohimban-16-carboxylic acid methyl ester
Percent Composition: C 71.16%, H 7.39%, N 7.90%, O 13.54%
Literature References: Present in the bark of Corynanthe johimbe K. Schum., Rubiaceae. Obtained from the residues of commercial isoln procedures for the manuf of yohimbine: Karrer, Salomon, Helv. Chim. Acta 9, 1059 (1926). Structure and stereochemistry: Janot et al., Bull. Soc. Chim. Fr. 1952, 1085; 1961, 637. Synthesis: van Tamelen et al., J. Am. Chem. Soc. 80, 5006 (1958); 91, 7315 (1969); Stork, Guthikonda, ibid. 94, 5109 (1972).

p-Aminopropiophenone CAS Registry Number: 70-69-9 4'-氨基苯丙酮

CAS Name: 1-(4-Aminophenyl)-1-propanone
Additional Names: ethyl p-aminophenyl ketone; PAPP
Percent Composition: C 72.46%, H 7.43%, N 9.39%, O 10.72%
Literature References: Pretreatment antidote to cyanide; activity probably through the formation of methemoglobin, which has a higher affinity for cyanide than mitochondrial cytochrome oxidase. Prepd by the action of propionyl chloride on aniline in carbon bisulfide in the presence of aluminum chloride: Kunckell, Ber. 33, 2641 (1900); Derrick, Bornemann, J. Am. Chem. Soc. 35, 1283 (1913); Hartung, Foster, J. Am. Pharm. Assoc. 35, 15 (1946). Antidotal activity: C. L. Rose et al., J. Pharmacol. Exp. Ther. 89, 109 (1947). Toxicity study: J. W. Scawin et al., Toxicol. Lett. 23, 359 (1984). Review of pharmacology of cyanide detoxification: S. I. Baskin, R. F. Fricke, Cardiovasc. Drug Rev. 10, 358-375 (1992).

Cilastatin CAS Registry Number: 82009-34-5 西司他丁

CAS Name: (2Z)-7-[[(2R)-2-Amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]carbonyl]amino]-2-heptenoic acidPercent Composition: C 53.61%, H 7.31%, N 7.82%, O 22.32%, S 8.95%
Literature References: Prevents renal metabolism of penem and carbapenem antibiotics by specific and reversible dehydropeptidase I inhibition. Synthesis and combination with thienamycins: D. W. Graham et al., EP 48301; H. Kropp et al., EP 48025 (both 1982 to Merck Co.), C.A. 97, 145271b, 145270a (1982). Combination with penems: F. M. Kahan, H. Kropp, EP 72014 (1983 to Merck Co.), C.A. 99, 70272h (1983). The articles cited below discuss the activity of cilastatin alone and in combination with imipenem, q.v. Dipeptidase inhibition, pharmacokinetics: S. R. Norrby et al., Antimicrob. Agents Chemother. 23, 300 (1983). Stimulation of granulocyte function: H. Gnarpe et al., ibid. 25, 179 (1984). HPLC determn in serum: C. M. Myers, J. L. Blumer, ibid. 26, 78 (1984). Enhances intrathecal and ocular penetration of imipenem: A. W. Chow et al., ibid. 23, 634 (1983) and K. R. Finlay et al., Invest. Ophthalmol. Visual Sci. 24, 1147 (1983), respectively. In experimental meningitis: D. E. Washburn et al., J. Antimicrob. Chemother. 12, 39 (1983). Series of articles on pharmacokinetics, safety and tolerance and efficacy of cilastatin/imipenem: ibid. 12, Suppl. D, 1-155 (1983); Infection 14, Suppl. 2, S111-S180 (1986).

Triethylborane CAS Registry Number: 97-94-9 三乙基硼

Additional Names: Triethylboron
Percent Composition: C 73.54%, H 15.43%, B 11.03%
Literature References: Primarily as an initiator in radical reactions. Prepn: A. Stock, F. Zeidler, Ber. 78, 531 (1921); E. C. Ashby, J. Am. Chem. Soc. 81, 4791 (1959). Use as protecting group: C. Lutz et al., Tetrahedron 54, 10317 (1998); as transfer reagent in polymerizations: V. Beraud et al., Macromol. Rapid Commun. 21, 901 (2000); as stereoselective intiator for hydrometalation: K. Takami et al., J. Org. Chem. 68, 6627 (2003). Review of radical reactivity in generation of carbon-centered radicals: C. Ollivier, P. Renaud, Chem. Rev. 101, 3415-3434 (2001). Brief review of application in radical initiation and in non-radical processes: G. O'Mahony, Synlett 2004, 572-573.

Quinine CAS Registry Number: 130-95-0 奎宁; 无水奎宁; 金鸡纳碱; 金鸡纳霜

CAS Name: (8a,9R)-6'-Methoxycinchonan-9-ol
Percent Composition: C 74.04%, H 7.46%, N 8.63%, O 9.86%
Literature References: Primary alkaloid of various species of Cinchona (Rubiaceae), see Cinchona. Representative samples of dried bark contain ~0.8 to 4% quinine. Optical isomer of quinidine, q.v. Isoln: Pelletier, Caventau, Ann. Chem. Phys. [2], 15, 291 (1820). Extraction procedure: Jucker, Stoll, in Ullmanns Encyklopädie der technischen Chemie vol. 3, 213-218 (1953). Configuration: Prelog, Zalán, Helv. Chim. Acta 27, 535 (1944); Prelog, Häfliger, ibid. 33, 2021 (1950); Roth, Pharmazie 16, 257 (1961). Synthesis: Woodward, Doering, J. Am. Chem. Soc. 66, 849 (1944); 67, 860 (1945); Taylor, Martin, ibid. 94, 6218 (1972); Gutzwiller, Uskokovic, ibid. 100, 576 (1978); G. Grethe et al., ibid. 589; T. Imanishi et al., Chem. Pharm. Bull. 30, 1925 (1982). Review of structural elucidation and early synthetic studies: R. B. Turner, R. B. Woodward in The Alkaloids vol. 3, 1-63 (1953); of bioactivity: F. E. Hahn, Ed. in Antibiotics vol. 5 (pt. 2) (Springer-Verlag, New York, 1979) pp 353-362. Comprehensive description of the hydrochloride: F. J. Muhtadi et al., Anal. Profiles Drug Subs. 12, 547-621 (1983). LC determn in soft drinks: L. P. Valenti, J. Assoc. Off. Anal. Chem. 68, 782 (1985). HPLC determn in blood: V. K. Dua et al. J. Chromatogr. 614, 87 (1993). Clinical evaluation to relieve nocturnal leg cramps: P. S. Connolly et al., Arch. Intern. Med. 152, 1877 (1992). Clinical efficacy in malaria: P. G. Kremsner et al., J. Infect. Dis. 169, 467-470 (1994). Review of historical importance and total syntheses: T. S. Kaufman, E. A. Ruveda, Angew. Chem. Int. Ed. 44, 854-885 (2005).

Methyl Nonyl Ketone CAS Registry Number: 112-12-9 2-十一酮; 甲基壬基甲酮

CAS Name: 2-Undecanone
Additional Names: 2-hendecanone
Percent Composition: C 77.58%, H 13.02%, O 9.40%
Literature References: Primary constituent of rue oils distilled mainly from Ruta montana L. and R. graveolens. Prepn: E. v. Gorup-Besanez, F. Grimm, Ann. 157, 275 (1871); V. Fiandanese et al., Tetrahedron Lett. 25, 4805 (1984); T. Aoyama, T. Shioiri, Synthesis 1988, 228. LC determn in formulations: R. J. Bushway, J. Assoc. Off. Anal. Chem. 73, 743 (1990). Physical properties: E. Guenther, D. Althausen, The Essential Oils vol. 2 (D. Van Nostrand, New York, 1949) p 377. Brief review: D. L. J. Opdyke, Food Cosmet. Toxicol. 13, 869-870 (1975).

Hyperforin CAS Registry Number: 11079-53-1 贯叶金丝桃素

CAS Name: (1R,5S,6R,7S)-4-Hydroxy-6-methyl-1,3,7-tris(3-methyl-2-butenyl)-5-(2-methyl-1-oxopropyl)-6-(4-methyl-3-pentenyl)bicyclo[3.3.1]non-3-ene-2,9-dione
Percent Composition: C 78.31%, H 9.76...
Literature References: Principal acylphloroglucinol component in St. John's wort with concentrations of 2-4% in the fresh herb. Inhibits synaptosomal uptake of serotonin, norephinephrine and dopamine; thought to be responsible for the antidepressant activity of medicinal preparations of hypericum, q.v. Isoln and antibacterial activity: A. I. Gurevich et al., Antibiotiki 16, 510 (1971), C.A. 75, 95625 (1971). Improved isoln procedure: C. A. J. Erdelmeier, Pharmacopsychiatry 31, Suppl 1, 2 (1998). Structure: N. S. Bystrov et al., Tetrahedron Lett. 1975, 2791. Abs config: I. Brondz et al., Acta Chem. Scand. A37, 263 (1983). HPLC determn in plasma: J. D. Chi, M. Franklin, J. Chromatogr. B 735, 285 (1999). Series of articles on psychopharmacology and neurotransmitter reuptake inhibition: Pharmacopsychiatry 31, Suppl 1, 7-29 (1998).

Allyl Isothiocyanate CAS Registry Number: 57-06-7 异硫氰酸烯丙酯

CAS Name: 3-Isothiocyanato-1-propene
Additional Names: isothiocyanic acid allyl ester; allyl isosulfocyanate; mustard oil; allyl mustard oil
Percent Composition: C 48.45%, H 5.08%, N 14.13%,...
Literature References: Principal constituent of volatile oil of mustard. Occurs in seeds as the glucoside, sinigrin, q.v. Isolated from Brassica nigra (L.) Koch, Cruciferae (black mustard seed), or prepd from allyl iodide and potassium thiocyanate: Dulière, J. Pharm. Belg. 2, 981 (1920), C.A. 15, 5714 (1921). Description: E. Guenther, D. Althausen, The Essential Oils vol. II (Van Nostrand, New York, 1949) pp. 734-7. Review of isolation: E. Guenther, ibid. vol VI, pp. 55-60 (1952); and synthesis: G. M. Dyson, Perfum. Essent. Oil Rec. 20, 42 (1929). Evaluation in relieving muscle pain: J. G. Macarthur, S. Alstead, Lancet 2, 1060 (1953). Toxicity study: P. M. Jenner et al., Food Cosmet. Toxicol. 2, 327 (1964). HPLC determn in brown mustard: K. Kanemaru et al., J. Jpn. Soc. Food Sci. Technol. 37, 565 (1990).

g -Irone CAS Registry Number: 79-68-5 4-(2,2,3-三甲基-6-亚甲基环己基)-3-丁烯-2-酮

CAS Name: 4-(2,2,3-Trimethyl-6-methylenecyclohexyl)-3-buten-2-one
Percent Composition: C 81.50%, H 10.75%, O 7.75%
Literature References: Principal fragrant constituent of natural iris oil. Isoln from irone mixture: Ruzicka et al., Helv. Chim. Acta 30, 1807 (1947); Ruzicka et al., ibid. 31, 257 (1948). Synthesis of dl-g-irone: Favre, Schinz, ibid. 41, 1368 (1958). Synthesis of (±)-cis- and trans-g-irone: F. Leyendecker, M.-T. Comte, Tetrahedron 43, 85 (1987); T. Kawanobe et al., Agric. Biol. Chem. 51, 791 (1987). Stereoselective synthesis of (±)-cis-g-irone: C. Nussbaumer, G. Fráter, Helv. Chim. Acta 71, 619 (1988). Stereochemistry: See a-irone.