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

Piribedil CAS Registry Number: 3605-01-4 吡贝地尔

CAS Name: 2-[4-(1,3-Benzodioxol-5-ylmethyl)-1-piperazinyl]pyrimidine
Additional Names: 2-(4-piperonyl-1-piperazinyl)pyrimidine; 2-[4-(3,4-methylenedioxybenzyl)piperazino]pyrimidine; 1-(2-pyrimi...
Literature References: Central dopaminergic agonist. Prepn: NL 6413349; G. Regnier et al., US 3299067; eidem, GB 1101425 (1965, 1967, 1968 all to Sci. Union et Cie-Soc. Franc. Rech. Med.); G. Regnier et al., J. Med. Chem. 11, 1151 (1968). Activity in man: R. Royer, Proc. 3rd Int. Pharmacol. Meet. 3, R. K. Richards, Ed. (Pergamon Press, New York, 1968) pp 45-55. Pharmacology: M. Laubie et al., Eur. J. Pharmacol. 6, 75 (1969). Metabolism: D. B. Campbell et al., Adv. Neurol. 3, 199 (1973). Review of mechanism of action: P. Jenner, J. Neurol. 239, Suppl. 1, S2-S8 (1992).

Guaifenesin CAS Registry Number: 93-14-1 愈创甘油醚

CAS Name: 3-(2-Methoxyphenoxy)-1,2-propanediol
Additional Names: glycerol mono(2-methoxyphenyl) ether; glycerol a-(2-methoxyphenyl) ether; guaiacyl glyceryl ether; glyceryl guaiacyl ether; glyc...
Literature References: Centrally acting muscle relaxant with expectorant properties. Prepn: Marle, J. Chem. Soc. 101, 305 (1912); Yale et al., J. Am. Chem. Soc. 72, 3710 (1950); Roviralta, Astoul, ES 212920 (1954), C.A. 49, 8332b (1955). Prepn from 2-methoxyphenol and glycidol: W. Merk et al., DE 3106995; eidem, US 4390732 (1982, 1983 to Degussa AG). GLC determn in blood: W. R. Maynard, R. B. Bruce, J. Pharm. Sci. 59, 1346 (1970). Clinical use in chronic respiratory disease: D. G. Workman et al., Curr. Ther. Res. 7, 665 (1965). Clinical efficacy as antitussive: J. J. Kuhn et al., Chest 82, 713 (1982). Pharmacokinetics and cardiopulmonary effects in horses: J. A. E. Hubbell et al., Am. J. Vet. Res. 41, 1751 (1980). Use in equine anesthesia: J. L. Grandy, W. N. McDonell, J. Am. Vet. Med. Assoc. 176, 619 (1980); G. J. Brouwer, Equine Vet. J. 17, 133 (1985).

Zoxazolamine CAS Registry Number: 61-80-3 苯并恶唑胺

CAS Name: 5-Chloro-2-benzoxazolamine
Additional Names: 2-amino-5-chlorobenzoxazoleTrademarks: Flexin (McNeil)
Percent Composition: C 49.87%, H 2.99%, Cl 21.03%, N 16.62%, O 9.49%
Literature References: Centrally acting myorelaxant; formerly used as an antispasmodic and uricosuric. Prepn: T. Nagana et al., J. Am. Chem. Soc. 75, 2770 (1953); J. Sam, US 2780633 (1957 to McNeil). Pharmacology and structure-activity studies: C. K. Cain, A. P. Roszkowski, "Benzoxazoles, Benzothiazoles and Benzimidazoles" in Medicinal Chemistry: A Series of Monographs 4, G. DeStevens, Ed. (Academic Press, New York, 1964) pp 325-357. Use in assay of microsomal oxidase activity: J. E. Tomaszeski et al., Arch. Biochem. Biophys. 176, 788 (1976). GLC determn and pharmacokinetics: M van der Graaff et al., Drug Metab. Dispos. 14, 331 (1986).

Cefdinir CAS Registry Number: 91832-40-5 头孢地尼

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(hydroxyimino)acetyl]amino]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: syn-7-[2-(2-amino-4-thiazolyl...
Literature References: Cephalosporin antibiotic structurally similar to cefixime, q.v. Prepn: T. Takaya et al., BE 897864; eidem, US 4559334 (1984, 1985 both to Fujisawa); Y. Inamoto et al., J. Antibiot. 41, 828 (1988); H. Kamachi et al., ibid. 1602. Improved prepn: M. González et al., Farmaco 58, 409 (2003). Clinical trial in children with acute otitis media: S. L. Block et al., Pediatr. Infect. Dis. J. 23, 834 (2004). Review of pharmacokinetics and in vitro antimicrobial activity: D. R. P. Guay, ibid. 19, S141-S146 (2000); of antibacterial activity, pharmacology and clinical efficacy: C. M. Perry, L. J. Scott, Drugs 64, 1433-1464 (2004).

Cephalonium CAS Registry Number: 5575-21-3 头孢洛宁

CAS Name: 4-(Aminocarbonyl)-1-[[(6R,7R)-2-carboxy-8-oxo-7-[(2-thienylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]pyridinium inner salt
Additional Names: cefalonium; 2-thienylme...
Literature References: Cephalosporin antibiotic. Prepn: E. H. Flynn, GB 1067644 (1967 to Lilly); and antibacterial activity: J. L. Spencer et al., Antimicrob. Agents Chemother. 1966, 573. Determn in milk samples: J. E. Hillerton et al., J. Dairy Sci. 82, 704 (1999). Prophylactic use in dry udder infections: R. Curtis et al., Vet. Rec. 100, 557 (1977); in mastitis: J. H. Williamson et al., N. Z. Vet. J. 43, 228 (1995); in combination with a teat sealer: M. W. Woolford et al., ibid. 46, 12 (1998).

Carfentrazone-ethyl CAS Registry Number: 128639-02-1 氟酮唑草

CAS Name: a-2-Dichloro-5-[4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1H-1,2,4-triazol-1-yl]-4-fluorobenzenepropanoic acid ethyl ester
Additional Names: ethyl 2-chloro-3-[2-chloro-4-fluoro-5-...
Literature References: Cereal herbicide that disrupts membranes by inhibiton of protoporphyrinogen oxidase. Prepn: K. M. Poss, WO 9002120 (1990 to FMC). Properties: W. A. Van Saun et al., Brighton Crop Prot. Conf. - Weeds 1993, 19. Synthesis and structure-activity: G. Theodoridis et al., ACS Symp. Ser. 584, 90 (1995). Mode of action: F. E. Dayan et al., Pestic. Sci. 51, 65 (1997). Control of broadleaf weeds in maize: S. F. Tutt et al., Brighton Crop Prot. Conf. - Weeds 1995 731; in wheat and barley: S. W. Shires et al., ibid. 1997, 117.

Phrenosin CAS Registry Number: 586-02-7 N-[(4E)-1-(beta-D-吡喃半乳糖基氧基)-3-羟基-4-十八碳烯-2-基]-2-羟基二十四n酰胺

CAS Name: (2R)-N-[(1S,2R,3E)-1-[(b-D-Galactopyranosyloxy)methyl]-2-hydroxy-3-heptadecenyl]-2-hydroxytetracosanamide
Percent Composition: C 69.61%, H 11.32%, N 1.69%, O 17.39%
Literature References: Cerebroside easily separated from a commercially available beef spinal cord lipid concentrate or from nerve tissue. A large proportion of its fatty acid content (25%) is 2-hydroxystearic acid, the rest is cerebronic (2-hydroxylignoceric) acid. Isoln: Radin et al., J. Biol. Chem. 219, 977 (1956); Skipski et al., Arch. Biochem. Biophys. 82, 487 (1959). Synthesis: Shapiro, Flowers, J. Am. Chem. Soc. 83, 3327 (1961).

Brovincamine CAS Registry Number: 57475-17-9 溴长春胺

CAS Name: (3a,14b,16a)-11-Bromo-14,15-dihydro-14-hydroxyeburnamenine-14-carboxylic acid methyl ester
Additional Names: cis-11-bromovincamine
Percent Composition: C 58.20%, H 5.81%, Br 18.44%...
Literature References: Cerebrovascular agent, vincamine deriv. Prepn: P. Pfaeffli, DE 2458164; idem, US 4146643 (1975, 1979 both to Sandoz). HPLC determn in plasma: R. R. Brodie, L. F. Chasseaud, J. Chromatogr. 228, 413 (1982). Effect on autonomic nervous system in laboratory animals: K. Kushiku et al., J. Pharmacobio-Dyn. 7, 177 (1984). Cardiovascular effects, mechanistic studies: eidem, Clin. Exp. Pharmacol. Physiol. 12, 121 (1985). Mode of action studies: T. Katsuragi et al., Gen. Pharmacol. 15, 43 (1984). Clinical trials in patients with multi-infarct dementia: S. Hagstadius et al., Psychopharmacology 83, 321 (1984).

Pinolenic Acid CAS Registry Number: 16833-54-8 皮诺敛酸

CAS Name: (5Z,9Z,12Z)-5,9,12-Octadecatrienoic acid
Percent Composition: C 77.65%, H 10.86%, O 11.49%
Literature References: Characteristic fatty acid of the seed oils of Pinus spp., Pinaceae. Positional isomer of g-linolenic acid, q.v. Isoln from tall oil: E. Elomaa et al., Suom. Kemistil. B 36, 52 (1963); A. Hase et al., J. Am. Oil Chem. Soc. 69, 832 (1992). Review of occurrence in the genus Pinus: R. L. Wolff et al., Lipids 35, 1-22 (2000). Effect of pinolenic acid-enriched pine nut oil on fatty acid metabolism in rats: M. Sugano et al., Br. J. Nutr. 72, 775 (1994); on LDL-receptor activity: J.-W. Lee et al., Lipids 39, 383 (2004).

Hypericin CAS Registry Number: 548-04-9 金丝桃素

CAS Name: 1,3,4,6,8,13-Hexahydroxy-10,11-dimethylphenanthro[1,10,9,8-opqra]perylene-7,14-dione
Additional Names: 4,5,7,4',5',7'-hexahydroxy-2,2'-dimethylnaphthodianthrone; hypericum red
Perc...
Literature References: Characteristic principal of hypericum, q.v. (St. John's wort). Isoln from Hypericum perforatum L., Hypericaceae: Brockmann et al., Ann. 553, 1 (1942). Synthesis from bromoemodin trimethylether: Brockmann, Muxfeld, Naturwissenschaften 40, 411 (1953). Structure: Brockmann et al., ibid. 37, 540 (1950); Brockmann, Sanne, ibid. 40, 509 (1953). Total synthesis: Brockmann, Kluge, US 2707704 (1955 to Schenley); Brockmann et al., Ber. 90, 2302 (1957); Brockmann, Eggers, ibid. 91, 547 (1958). Clinical pharmacokinetics and evaluation of phototoxic potential: J. Brockmöller et al., Pharmacopsychiatry 30, Suppl 2, 94 (1997). HPLC determn in plasma: J. D. Chi, M. Franklin, J. Chromatogr. B 724, 195 (1999).