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

Pirozadil CAS Registry Number: 54110-25-7 吡扎地尔

CAS Name: 3,4,5-Trimethoxybenzoic acid 2,6-pyridinediylbis(methylene)ester
Additional Names: 2,6-pyridinedimethanol bis(3,4,5-trimethoxybenzoate)Trademarks: Pemix (Prodes)
Percent Compositio...
Literature References: Hypolipidemic agent that inhibits platelet aggregation. Prepn: J. P. Cochs, DE 2411902 (1974 to Inst. Int. Ter.), C.A. 82, 4136q (1975). Effect on cerebral metabolic blood flow in rabbits: J. Balasch, L. Palacios, Arch. Farmacol. Toxicol. 3, 137 (1977). Efficacy in exptl atherosclerosis: M. R. Parwaresch et al., Atherosclerosis 31, 395 (1978). Toxicological and histopathological study: J. Roca et al., Arch. Farmacol. Toxicol. 6, 41 (1980). Clinical trials in hyperlipoproteinemia: M. Shinomiya et al., Arzneim.-Forsch. 37, 1069 (1987); R. Tapounet, I. Marti Ragué, Drugs Exp. Clin. Res. 13, 447 (1987).

Diazoxide CAS Registry Number: 364-98-7 氯甲苯噻嗪

CAS Name: 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
Additional Names: 3-methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxideTrademarks: Eudemine Injection (Schering); Proglicem (Ess...
Literature References: Hypotensive agent that inhibits secretion of insulin from pancreatic beta cells. Prepn: A. A. Rubin et al., Science 133, 2067 (1961); J. G. Topliss et al., US 2986573; eidem, US 3345365 (1961, 1967 both to Schering); Raffa, Monzani, Farmaco Ed. Sci. 17, 244 (1962). Crystal and molecular structure: G. Bandoli, M. Nicolini, J. Cryst. Mol. Struct. 7, 229 (1978). Review of effect on insulin secretion: Nutr. Rev. 30, 194-198 (1972); of pharmacology and efficacy in hypertension: J. Koch-Weser, N. Engl. J. Med. 294, 1271-1274 (1976).

Guanazodine CAS Registry Number: 32059-15-7 2-(氮杂环辛烷-2-基甲基)胍硫酸盐

CAS Name: [(Octahydro-2-azocinyl)methyl]guanidine
Additional Names: a-guanidinomethylheptamethylenimine; 1-azacyclooct-2-ylmethylguanidine
Percent Composition: C 58.66%, H 10.94%, N 30.40%
Literature References: Hypotensive agent, related structurally to guanethidine. Prepn of the sulfate salt: J. Rakoczi et al., HU 155990; eidem, US 3856778 (1969, 1974 both to EGYT). Pharmacokinetics in man: T. Past et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 8, 111 (1973). General pharmacology: H. Iwata et al., Oyo Yakuri 14, 235 (1977), C.A. 88, 16070 (1977). Analytical study: E. Zollner-Ivan, Acta Pharm. Hung. 48, 76 (1978). Clinical studies in hypertension: S. Dobi et al., Ther. Hung. 28, 60 (1980); Z. Herpai et al., ibid. 181.

Elenolide CAS Registry Number: 24582-91-0 甲基(4S)-2-氧代-4-[(2E)-1-氧代-2-丁烯-2-基]-3,4-二氢-2H-吡喃-5-羧酸酯

CAS Name: (4S)-4-[(1E)-1-Formyl-1-propenyl]-3,4-dihydro-2-oxo-2H-pyran-5-carboxylic acid methyl ester
Percent Composition: C 58.93%, H 5.39%, O 35.68%
Literature References: Hypotensive lactone from fruits, bark and leaves of the olive tree, Olea europaea L., Oleaceae: Veer et al., Rec. Trav. Chim. 76, 839 (1957); GB 789427 (1958 to Organon); US 3033877 (1962 to Organon). Structure: Panizzi et al., Gazz. Chim. Ital. 90, 1464 (1960); Beyerman et al., Bull. Soc. Chim. Fr. 1961, 1812. Synthesis from secologanin: L. F. Tietze, H. C. Uzar, Angew. Chem. Int. Ed. 18, 539 (1979).

CRF CAS Registry Number: 9015-71-8 CRF1受体激动剂

CAS Name: Corticotropin-releasing factor
Additional Names: CRH; corticoliberin(e); corticotropin-releasing hormone
Literature References: Hypothalamic substance that stimulates secretion of ACTH, q.v. and b-endorphin from the pituitary. First direct evidence for its presence in hypothalami: R. Guillemin, B. Rosenberg, Endocrinology 57, 599 (1955); M. Saffran, A. V. Schally, Can. J. Biochem. Physiol. 33, 408 (1955). Purification and characterization of a 41-residue ovine hypothalamic CRF that is highly potent in stimulating secretion of corticotropin and b-endorphin-like immunoactivities: W. Vale et al., Science 213, 1394 (1981). Primary structure: J. Spiess et al., Proc. Natl. Acad. Sci. USA 78, 6517 (1981). When centrally administered, CRF activates the sympathetic nervous system and may therefore function as a key hormone in stress mobilization of the organism, cf. W. Vale et al., loc. cit.; M. Brown et al., Life Sci. 30, 207 (1982). CRF also stimulates a-MSH secretion and cyclic AMP accumulation in rat pars intermedia cells: H. Meunier et al., ibid. 31, 2129 (1982). A functional relationship between CRF and dynorphin-related opioid peptides has also been suggested: K. A. Roth et al., Science 219, 189 (1983). Reviews: A. V. Schally et al., Recent Prog. Horm. Res. 24, 497-588 (1968); R. Burgus, R. Guillemin, Annu. Rev. Biochem. 39, 499-526 (1970); M. Saffran in Hypothalamic Peptide Hormones and Pituitary Regulation, J. C. Porter, Ed. (Plenum Press, New York, 1977) pp 225-235; W.Vale et al. in The Role of Peptides in Neuronal Function, J. L. Barker, J. G. Smith, Eds. (Dekker, New York, 1980) pp 432-454; several authors in Polypeptide Hormones, R. F. Beers, E. G. Bassett, Eds. (Raven Press, New York, 1980) pp 165-271; B. Lutz-Bucher et al., J. Physiol. 77, 939-950 (1981); N. Yasuda et al., Endocr. Rev. 3, 123-140 (1982); E. Stark, G. B. Makara in Hormonally Active Brain Peptides: Structure and Function, K. W. McKerns, V. Pantic, Eds. (Plenum Press, New York, 1982) pp 157-179.

Didanosine CAS Registry Number: 69655-05-6 地达诺辛

CAS Name: 2',3'-Dideoxyinosine
Additional Names: dideoxyinosine; ddI; ddInoTrademarks: Videx (BMS)
Percent Composition: C 50.84%, H 5.12%, N 23.72%, O 20.32%
Literature References: Hypoxanthine nucleoside with antiviral activity; metabolic product of dideoxyadenosine, q.v. Enzymatic prepn from dideoxyadenosine: W. Plunkett, S. S. Cohen, Cancer Res. 35, 1547 (1975). Synthesis: G. W. Koszalka, T. A. Krenitsky, EP 206497 (1986 to Wellcome Found.); R. R. Webb et al., Nucleosides Nucleotides 7, 147 (1988). In vitro inhibition of HIV-I: H. Mitsuya, S. Broder, Proc. Natl. Acad. Sci. USA 83, 1911 (1986); of HIV-II: D. D. Richman, Antimicrob. Agents Chemother. 31, 1879 (1987). Antiretroviral spectrum in vitro: J. E. Dahlberg et al., Proc. Natl. Acad. Sci. USA 84, 2469 (1987). Cellular pharmacology in cloned human T-cells: G. Ahluwalia et al., Biochem. Pharmacol. 36, 3797 (1987). HPLC determn in human plasma: G. Ray, E. Murrill, Anal. Lett. 20, 1815 (1987). Clinical evaluations in AIDS: J. S. Lambert et al., N. Engl. J. Med. 322, 1333 (1990); T. P. Cooley et al., ibid. 1340. Comprehensive description: M. N. Nassar et al., Anal. Profiles Drug Subs. Excip. 22, 185-227 (1993).

Imipramine N-Oxide CAS Registry Number: 6829-98-7 氧丙咪嗪

CAS Name: 10,11-Dihydro-N,N-dimethyl-5H-dibenz[b,f]azepine-5-propanamine N-oxide
Additional Names: 5-[3-(dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine N-oxide; N-(g-dimethylaminopro...
Literature References: Identification as a metabolite of imipramine, q.v.: V. Fishman, H. Goldenberg, Proc. Soc. Exp. Biol. Med. 110, 187 (1962). Prepn: FR M2508; H. Dyrsting, J. B. Pedersen, US 3574852 (1964, 1971, both to Dumex). Pharmacology: W. Theobald et al., Med. Pharmacol. Exp. 15, 187 (1966). Metabolism: M. H. Bickel, M. Baggiolini, Biochem. Pharmacol. 15, 1155 (1966); R. Minder et al., Arch. Pharmakol. 268, 334 (1971). GLC determn in biological samples: H. J. Weder, M. H. Bickel, J. Chromatogr. 37, 181 (1968); HPLC determn: E. Koyama et al., Ther. Drug Monit. 15, 224 (1993). Clinical trial: W. Rapp et al., Acta Psychiatr. Scand. 49, 77 (1973). Clinical pharmacokinetics: A. Nagy, T. Hansen, Acta Pharmacol. Toxicol. 42, 58 (1978).

Flumazenil CAS Registry Number: 78755-81-4 氟吗西尼

CAS Name: 8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester
Additional Names: ethyl-8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,...
Literature References: Imidazodiazepine which selectively blocks the central effects of classic benzodiazepines. Prepn: W. Haefely et al., EP 27214; M. Gerecke et al., US 4316839 (1981, 1982 both to Hoffmann-La Roche). Specific inhibition of benzodiazepine-receptor binding: W. Hunkeler et al., Nature 290, 514 (1981). Electrophysiological study in animals: P. Pole et al., Arch. Pharmacol. 316, 317 (1981). Antagonist, agonist and inverse agonist properties: S. E. File et al., Psychopharmacology 89, 113 (1986). HPLC determn in human plasma: U. Timm, M. Zell, Arzneim.-Forsch. 33, 358 (1983). Clinical reversal of benzodiazepine-induced sedation: A. Darragh et al., Lancet 2, 8 (1981); eidem, ibid. 1042; B. Ricou et al., Br. J. Anaesth. 58, 1005 (1986). Clinical evaluation in drug overdose: G. F. O'Sullivan et al., Clin. Pharmacol. Ther. 42, 254 (1987).

Nizofenone CAS Registry Number: 54533-85-6 尼唑苯酮

CAS Name: (2-Chlorophenyl)[2-[2-[(diethylamino)methyl]-1H-imidazol-1-yl]-5-nitrophenyl]methanone
Additional Names: 2'-chloro-2-[2-[(diethylamino)methyl]imidazol-1-yl]-5-nitrobenzophenone; 1-[2-...
Literature References: Imidazole derivative exhibiting protective activity against cerebral anoxia or ischemia. Prepn: M. Nakanishi et al., DE 2403416; eidem, US 3915981 (1974, 1975 both to Yoshitomi). Antianoxic effect in animal models: H. Yasuda et al., Arch. Int. Pharmacodyn. 233, 136 (1978). Mechanism of action: eidem, ibid. 242, 77 (1979). Multicenter clinical studies: I. Saito et al., Neurol. Res. 5, 29 (1983); T. Ohta et al., J. Neurosurg. 64, 420 (1986). Toxicity studies: H. Horizoe et al., Oyo Yakuri 30, 627 (1985), C.A. 104, 61754m (1986); K. Okumura et al., ibid. 633, C.A. 104, 61755 (1986).

Capravirine CAS Registry Number: 178979-85-6 2-氨基甲酰氧基甲基-5-(3,5-二氯苯基硫代)-4-异丙基-1-(吡啶-4-基)甲基-1H-咪唑

CAS Name: 5-[(3,5-Dichlorophenyl)thio]-4-(1-methylethyl)-1-(4-pyridinylmethyl)-1H-imidazole-2-methanol carbamate ester
Additional Names: 2-carbamoyloxymethyl-5-(3,5-dichlorophenylthio)-4-isopro...
Literature References: Imidazole type non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI). Prepn: H. Sugimoto, T. Fujiwara, WO 9610019; eidem, US 5910506 (1996, 1999 both to Shionogi). Antiviral activity: T. Fujiwara et al., Antimicrob. Agents Chemother. 42, 1340 (1998). Crystal structure in complex with target enzyme: J. Ren et al., J. Biol. Chem. 275, 14316 (2000). Review of pharmacology and clinical evaluation: W. M. Brown, Curr. Opin. Anti-Infect. Invest. Drugs 2, 286-294 (2000).