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

Pazinaclone CAS Registry Number: 103255-66-9 帕秦克隆

CAS Name: 8-[[2-(7-Chloro-1,8-naphthyridin-2-yl)-2,3-dihydro-3-oxo-1H-isoindol-1-yl]acetyl]-1,4-dioxa-8-azaspiro[4.5]decane
Additional Names: (±)-2-(7-chloro-1,8-naphthyridin-2-yl)-3-[(1,4...
Literature References: Non-benzodiazepine exhibiting mixed agonist/antagonist effects with benzodiazepine receptors; activity resides primarily in the (S)-enantiomer. Prepn: G. Goto, Y. Saji, EP 174858; eidem, US 4695572 (1986, 1987 both to Takeda). Pharmacologic profile: T. Wada, N. Fukuda, Psychopharmacology 103, 314 (1991). HPLC determn in human plasma and urine, of racemate and/or its metabolites: Z. Hussein et al., J. Chromatogr. 613, 105 (1993); of enantiomers and/or their metabolites: eidem, ibid. 113. Clinical pharmacokinetics of racemate and its enantiomers: Z. Hussein et al., Br. J. Clin. Pharmacol. 36, 357 (1993). Clinical evaluation and abuse liability of racemate: G. K. Mumford et al., Exp. Clin. Psychopharmacol. 3, 39 (1995).

Alpidem CAS Registry Number: 82626-01-5 阿尔吡登

CAS Name: 6-Chloro-2-(4-chlorophenyl)-N,N-dipropylimidazo[1,2-a]pyridine-3-acetamideTrademarks: Ananxyl (Synthelabo)
Percent Composition: C 62.38%, H 5.73%, Cl 17.54%, N 10.39%, O 3.96%
Literature References: Non-benzodiazepine tranquilizer. Prepn: J. P. Kaplan, P. George, EP 50563; eidem, US 4382938 (1982, 1983 both to Synthelabo). Pharmacology and pharmacokinetics in humans: B. Saletu et al., Int. Clin. Psychopharmacol. 1, 145 (1986). HPLC determn in human plasma: V. Ascalone et al., J. Chromatogr. 414, 101 (1987). Clinical evaluation of tranquilizing vs hypnotic effects: B. Saletu et al., Curr. Ther. Res. 40, 769 (1986). Pilot study in anxiety: S. F. Langer et al., Psychopharmacol. Bull. 24, 161 (1988). Hepatotoxicity in rats: A. Berson et al., J. Pharmacol. Exp. Ther. 299, 793 (2001).

Sobuzoxane CAS Registry Number: 98631-95-9 索布佐生

CAS Name: 1,2-Ethanediylbis[(2,6-dioxo-4,1-piperazinediyl)methylene]carbonic acid bis(2-methylpropyl) ester
Additional Names: 4,4'-ethylenebis[1-(hydroxymethyl)-2,6-piperazinedione] bis(isobuty...
Literature References: Noncleavable complex-stabilizing DNA topoisomerase II inhibitor. Prepn: J.-C. Cai, M. Takase, EP 140327; eidem, US 4650799 (1985, 1987 both to Zenyaku Kogyo); idem et al., Chem. Pharm. Bull. 37, 2976 (1989). Antitumor activity: T. Narita et al., Cancer Chemother. Pharmacol. 28, 235 (1991). Clinical evaluation in non-Hodgkin's lymphoma: R. Ohno et al., J. Natl. Cancer Inst. 84, 435 (1992); in adult T-cell leukemia-lymphoma: idem et al., Cancer 71, 2217 (1993). Acute toxicity study: T. Tokiwa et al., Iyakuhin Kenkyu 22, 435 (1991). C.A. 115, 222916k (1991).

Talampanel CAS Registry Number: 161832-65-1 (8R)-7-乙酰基-5-(4-氨基苯基)-8,9-二氢-8-甲基-7H-1,3-二氧杂环戊烯并[4,5-H][2,3]苯并二氮杂卓

CAS Name: (8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine
Additional Names: R-(-)-1-(4-aminophenyl)-3-acetyl-4-methyl-7,8-methylenedioxy-3,4-dihydr...
Literature References: Noncompetitive AMPA receptor antagonist. Prepn: F. Andrasi et al., EP 492485; eidem, US 5536832 (1992, 1996 both to Gyogyszerkutato Intezet KFT). Enantioselective synthesis: I. Ling et al., J. Chem. Soc. Perkin Trans. 1 1995, 1423. HPLC determn in plasma: J. A. Eckstein, S. P. Swanson, J. Chromatogr. B 668, 153 (1995). Stereoselective electropharmacology and neuroprotective effects: D. Lodge et al., Neuropharmacology 35, 1681 (1996). Review of manufacturing process: B. A. Anderson et al. in Process Chemistry in the Pharmaceutical Industry, K. G. Gadamasetti, Ed. (Marcel Dekker, New York, 1999) pp 263-282. Review of clinical development: C. Q. Meng, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 1, 637-643 (1999).

Dizocilpine CAS Registry Number: 77086-21-6 地佐环平

CAS Name: 10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
Additional Names: (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine
Percent Composition: C 86.84%, H 6.8...
Literature References: Non-competitive NMDA, q.v., receptor antagonist. Prepn of racemate: M. E. Christy et al., J. Org. Chem. 44, 3117 (1979); T. R. Lamanec et al., ibid. 53, 1768 (1988); and of enantiomers: BE 882361; P. Anderson et al., US 4399141 (1980, 1983 both to Merck Co.). Series of papers on pharmacological activities: B. V. Clineschmidt et al., Drug Dev. Res. 2, 123-163 (1982). NMDA receptor binding studies: E. H. F. Wong et al., Proc. Natl. Acad. Sci. USA 83, 7104 (1986); A. C. Foster, E. H. F. Wong, Br. J. Pharmacol. 91, 403 (1987); J. E. Huettner, B. P. Bean, Proc. Natl. Acad. Sci. USA 85, 1307 (1988). Metabolism in animals: H. B. Hucker et al., Drug Metab. Dispos. 11, 54 (1983). Pharmacokinetics: A. S. Troupin et al., Curr. Probl. Epilepsy 4, 191 (1986). Protective effects against excitotoxic amino acid-induced neuronal degeneration: G. N. Woodruff et al., Neuropharmacology 26, 903 (1987); A. C. Foster et al., Neurosci. Lett. 76, 307 (1987); A. C. Foster et al., J. Neurosci. 8, 4745 (1988); specifically in ischemia: R. Gill et al., Neuroscience 25, 847 (1988); E. Ozyurt et al., J. Cereb. Blood Flow Metab. 8, 138 (1988). Anticonvulsant activity in models of epilepsy: K. Sato et al., Brain Res. 463, 12 (1988); M. E. Gilbert, ibid. 90. Clinical evaluation in attention deficit disorder: F. W. Reimherr et al., Psychopharmacol. Bull. 22, 237 (1986).

Aptiganel CAS Registry Number: 137159-92-3 1-(3-乙基苯基)-1-甲基-2-萘-1-基胍

CAS Name: N-(3-Ethylphenyl)-N-methyl-N'-1-naphthalenylguanidine
Additional Names: N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine; aptaguanal
Percent Composition: C 79.17%, H 6.98%, N 1...
Literature References: Noncompetitive NMDA-receptor antagonist. Prepn: E. Weber, J. F. W. Keana, WO 9112797; eidem, US 5262568 (1991, 1993 both to State of Oregon); N. L. Reddy et al., J. Med. Chem. 37, 260 (1994). Clinical pharmacology and kinetics: K. W. Muir et al., Ann. N.Y. Acad. Sci. 765, 279 (1995). Review of theoretical basis for use in stroke: K. W. Muir, K. R. Lees, Stroke 26, 503-513 (1995). Clinical trial in acute ischemic stroke: G. W. Albers et al., J. Am. Med. Assoc. 286, 2673 (2001).

Mivacurium Chloride CAS Registry Number: 106861-44-3 米库氯铵

CAS Name: (1R,1'R)-2,2'-[[(4E)-1,8-Dioxo-4-octene-1,8-diyl]bis(oxy-3,1-propanediyl)]bis[1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-[(3,4,5-trimethoxyphenyl)methyl]]isoquinolinium dichloride
Ad...
Literature References: Non-depolarizing neuromuscular blocking agent. Prepn: R. A. Swaringen, Jr. et al., DD 235638; eidem, US 4761418 (1986, 1988 both to Burroughs Wellcome). Clinical pharmacology: H. H. Ali et al., Br. J. Anaesth. 61, 541 (1988); J. J. Savarese et al., Anesthesiology 68, 723 (1988). In vitro metabolism: D. R. Cook et al., Anesth. Analg. 68, 452 (1989). Clinical evaluation in adults: S. Weber et al., ibid. 67, 495 (1988); R. P. From et al., Br. J. Anaesth. 64, 193 (1990); in children: J. K. Alifimoff, N. G. Goudsouzian, ibid. 63, 520 (1989).

Quinagolide CAS Registry Number: 87056-78-8 喹高利特

CAS Name: (3R,4aR,10aS)-rel-N,N-Diethyl-N'-(1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propylbenzo[g]quinolin-3-yl)sulfamide
Additional Names: (±)-1-n-propyl-3a-diethylsulfamoylamino-6-hydr...
Literature References: Nonergot dopamine D2-receptor agonist. Prepn: R. Nordmann, T. J. Petcher, EP 77754; eidem, US 4565818 (1983, 1986 both to Sandoz); eidem, J. Med. Chem. 28, 367 (1985). Receptor binding study in vivo: A. Closse et al., Brain Res. 440, 123 (1988). Clinical pharmacology: R. C. Gaillard, J. Brownell, Life Sci. 43, 1355 (1988). Clinical evaluation in hyperprolactinemia: C. Rasmussen et al., Acta Endocrinol. 125, 170 (1991).

Asparagine CAS Registry Number: 70-47-3 L-天冬酰胺

CAS Name: L-Asparagine
Additional Names: Asn; N; L-b-asparagine; a-aminosuccinamic acid; aspartic acid b-amide; altheine; asparamide; agedoite; (S)-2,4-diamino-4-oxobutanoic acid
Percent Com...
Literature References: Non-essential amino acid for human development. First amino acid noted in natural sources, it was named for the asparagus juice from which it was isolated: L. N. Vauquelin, P. J. Robiquet, Ann. Chim. 57, 88 (1806). Due to ease of conversion to aspartic acid, q.v., it was not isolated from protein until 1932: M. Damodoran, Biochem. J. 26, 235 (1932). Early chemistry and biochemistry: Amino Acids and Proteins, D. M. Greenberg, Ed. (Charles C. Thomas, Springfield, IL, 1951) 950 pp, passim; J. P. Greenstein, M. Winitz, Chemistry of the Amino Acids vols. 1-3 (John Wiley Sons, Inc., New York, 1961) pp. 1856-1878, passim. As attachment point for saccharides: A. J. Mencke et al., Methods Enzymol. 138, 409 (1987). Colorimetric assay: S. Sheng et al., Anal. Biochem. 211, 242 (1993). Proposed formation of acrylamide, q.v., in cooking: D. S. Mottram et al., Nature 419, 448 (2002); R. H. Stadler et al., ibid. 449. Review of metabolism: D. A. Cooney, R. E. Handschumacher, Annu. Rev. Pharmacol. 10, 421-440 (1970); in plants: K. A. Sieciechowicz et al., Phytochemistry 27, 663-671 (1988). Review of deamidation in proteins: R. Bischoff, H. V. J. Kolbe, J. Chromatogr. B 662, 261-278 (1994).

Aspartic Acid CAS Registry Number: 56-84-8 L-天门冬氨酸

CAS Name: L-Aspartic acid
Additional Names: Asp; D; aminosuccinic acid; asparagic acid; asparaginic acid; (S)-aminobutanedioic acid; 1-amino-1,2-carboxyethane; asparaginsäure (German)
Percen...
Literature References: Non-essential amino acid for human development. First identified as the acid hydrolysis product of asparagine, q.v.: A. Plisson, J. Pharm. 13, 477 (1827); later isolated from protein: H. Ritthausen, J. Prakt. Chem. 103, 233, 239 (1868). Early chemistry and biochemistry: Amino Acids and Proteins, D. M. Greenberg, Ed. (Charles C. Thomas, Springfield, IL, 1951) 950 pp., passim; J. P. Greenstein, M. Winitz, Chemistry of the Amino Acids vol 1-3 (John Wiley and Sons, Inc., New York, 1961) pp. 1856-1878, passim. Synthesis of optically active forms: K. Harada, K. Matsumoto, J. Org. Chem. 31, 2985 (1966); of labelled form: A. Ivanof et al., Anal. Biochem. 110, 267 (1981). Crystal structure: B. Dawson, Acta Crystallogr. 33B, 882 (1977). Excitatory neurotransmitter: H. McLennan, H. V. Wheal, Can. J. Physiol. Pharmacol. 54, 70 (1976). Role in protein activity: D. W. Urry et al., Biopolymers 34, 889 (1994); J. M. Denu et al., Biochemistry 34, 3396 (1995). Racemization with age in dentin: N. Saleh et al., Calcif. Tissue Int. 53, 103 (1993). Review of metabolism and pathology: L. D. Stegink, J. Toxicol. Environ. Health 2, 215-242 (1976). Review of role as excitatory amino acid: P. J. Roberts, S. W. Davies, Biochem. Soc. Trans. 15, 218-219 (1986); of use in forensics: E. R. Waite et al., Forensic Sci. Int. 103, 113-124 (1999); of pathobiology of age-related racemization in proteins: S. Ritz-Timme, M. J. Collins, Ageing Res. Rev. 1, 43-59 (2002).