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

Indenolol CAS Registry Number: 60607-68-3 茚诺洛尔

CAS Name: 1-[1H-Inden-4(or 7)-yloxy]-3-[(1-methylethyl)amino]-2-propanol
Additional Names: (±)-1-[inden-4(or 7)-yloxy]-3-(isopropylamino)-2-propanolPercent Composition: C 72.84%, H 8.56%, ...
Literature References: Non-selective b-adrenergic blocker. Prepn: M. Murakami et al., DE 1955229; eidem, US 4045482 (1970, 1977 both to Yamanouchi); K. Murase et al., Yakugaku Zasshi 92, 1358 (1972), C.A. 78, 71723 (1973). Indenolol is a tautomeric mixture of the 7- and 4-indenyloxy isomers in a 2:1 ratio, respectively. Unambiguous synthesis of the two isomers: eidem, Chem. Pharm. Bull. 24, 552 (1976). b-Blocking and cardiovascular properties: T. Takenaka, S. Tachikawa, Arzneim.-Forsch. 22, 1864 (1972). General pharmacology: M. Takeda et al., Oyo Yakuri 7, 469 (1973), C.A. 80, 44015 (1974). Comparative pharmacological study with other b-blockers: W. Bartsch et al., Arzneim.-Forsch. 27, 1022 (1977). Dose-response studies: F. E. Okupa et al., Clin. Pharmacol. Ther. 29, 434 (1981). Pharmacokinetics: R. Sega et al., J. Clin. Pharmacol. 25, 337 (1985). Clinical evaluation in hypertension: B. Trimarco et al., ibid. 328; L. Poggesi et al., Clin. Pharmacol. Ther. 41, 344 (1987).

Xibenolol CAS Registry Number: 81584-06-7 希苯洛尔

CAS Name: 1-[(1,1-Dimethylethyl)amino]-3-(2,3-dimethylphenoxy)-2-propanol
Additional Names: 3-(tert-butylamino)-3-(2',3'-dimethylphenoxy)-2-propanol; (±)-1-(tert-butylamino)-3-(2,3-xylylox...
Literature References: Non-selective b-adrenergic blocker. Prepn: W. Kunz et al., DE 1236523 (1967 to Sanol-Arzneimittel), C.A. 67, 64046k (1967); K. Tsukamoto et al., US 4018824 (1977 to Teikoku Hormone). Pharmacology in dogs: N. Himori et al., Arch. Int. Pharmacodyn. 220, 4 (1976); eidem, Arch. Pharmacol. 316, 19 (1986). Metabolism in animals: S. Honma, A. Kambekawa, Chem. Pharm. Bull. 23, 1045 (1975). Stereoselective metabolism and pharmacokinetics in man: S. Honma et al., ibid. 33, 760 (1985). Toxicology: T. Usui et al., Yakuri to Chiryo 12, Suppl. 6, 969, 987 (1984); C.A. 102, 125280x, 125281y (1985).

Levobunolol CAS Registry Number: 47141-42-4 左布诺洛尔

CAS Name: 5-[(2S)-3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-1(2H)-naphthalenone
Additional Names: (-)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1(2H)-naphthalenone; ...
Literature References: Nonselective b-adrenoceptor antagonist. Prepn of racemate: C. F. Schwender et al., J. Med. Chem. 13, 684 (1970); J. Shavel, Jr., S. Farber, DE 1948144; eidem, US 3641152 (1970, 1972 both to Warner-Lambert). Resolution of enantiomers: J. Shavel, Jr., C. F. Schwender, DE 2046043; eidem, US 3649691 (1971, 1972 both to Warner-Lambert); R. D. Dennis et al., US 4463176 (1984 to Bristol Myers, Mead Johnson). Cardiovascular pharmacology, anti-arrhythmic activity of racemate and isomers: R. D. Robson, H. R. Kaplan, J. Pharmacol. Exp. Ther. 175, 157, 168 (1970). Adrenoceptor blocking activity: H. R. Kaplan et al., Eur. J. Pharmacol. 16, 237 (1971). Metabolism in humans: F. J. DiCarlo et al., Clin. Pharmacol. Ther. 22, 858 (1977); F.-J. Leinweber et al., Pharmacology 16, 70 (1978). Corneal permeability: R. D. Schoenwald, H.-S. Huang, J. Pharm. Sci. 72, 1266, 1272 (1983). HPLC determn in biological fluids: H. Hengy, E. U. Kolle, J. Chromatogr. 338, 444 (1985); D. D. S. Tang-Liu et al., J. Liq. Chromatogr. 9, 2237 (1986). Clinical evaluation in hypertension: E. Arce-Gomez et al., Curr. Ther. Res. 19, 386 (1976); comparison with timolol, q.v., in glaucoma and ocular hypertension: A. Cinotti et al., Am. J. Ophthalmol. 99, 11 (1985); D. Long et al., ibid. 18. Review: H. R. Kaplan, "Levobunolol" in Pharmacology of Antihypertensive Drugs, A. Scriabine, Ed. (Raven Press, New York, 1980) pp 317-323. Brief review of long-term treatment of glaucoma: G. D. Novack, Gen. Pharmacol. 17, 373-377 (1986).

Amitrole CAS Registry Number: 61-82-5 3-氨基-1,2,4-三唑

CAS Name: 1H-1,2,4-Triazol-3-amine
Additional Names: 3-amino-1H-1,2,4-triazole; aminotriazole; ATATrademarks: Amizol (CFPI); Cytrol; Weedazol (CFPI)
Percent Composition: C 28.57%, H 4.80%, N...
Literature References: Non-selective post-emergence, translocated herbicide. Prepn: G. Sjostedt, L. Gringas, Org. Synth. coll. vol. III, 95 (1955). Use as herbicide: Allen, US 2670282 (1954 to Am. Chemical Paint Co.). Antithyroid activity: T. H. Jukes, C. B. Shaffer, Science 132, 296 (1960). Review: E. Kröller, Residue Rev. 12, 163-192 (1966). Review of carcinogenicity studies: IARC Monographs 7, 31-43 (1974).

Nifekalant CAS Registry Number: 130636-43-0 尼非卡兰

CAS Name: 6-[[2-[(2-Hydroxyethyl)[3-(4-nitrophenyl)propyl]amino]ethyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione
Percent Composition: C 56.28%, H 6.71%, N 17.27%, O 19.73%
Literature References: Nonselective potassium channel blocker. Prepn: T. Katakami et al., EP 369627; eidem, US 5008267 (1990, 1991 both to Mitsui Toatsu Chem.); eidem, J. Med. Chem. 35, 3325 (1992). Pharmacology: J. Kamiya et al., Drug Dev. Res. 30, 37 (1993). Clinical experience: M. Igawa et al., J. Cardiovasc. Pharmacol. 40, 735 (2002); T. Minami et al., Pacing Clin. Electrophysiol. 27, 212 (2004). Review of pharmacology: H. Nakaya, H. Uemura, Cardiovasc. Drug Rev. 16, 133-144 (1998); of development and therapeutic potential: A. Zaza, Curr. Opin. Cardiovasc. Pulm. Renal Invest. Drugs 2, 86-94 (2000). Clinical evaluation in ventricular tachyarrhythmias: T. Katoh et al., Circ. J. 69, 1237 (2005); T. Washizuka et al., ibid. 1508; in shock-refractory ventricular fibrillation: Y. Tahara et al., ibid. 70, 442 (2006).

Sulfometuron-methyl CAS Registry Number: 74222-97-2 甲嘧磺隆

CAS Name: 2-[[[[(4,6-Dimethyl-2-pyrimidinyl)amino]carbonyl]amino]sulfonyl]benzoic acid methyl ester
Additional Names: N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulfo...
Literature References: Nonselective pre- and post-emergence sulfonylurea herbicide for noncropland use; inhibits branched chain amino acid biosynthesis. Prepn: G. Levitt, EP 7687; idem, US 4394506 (1980, 1983 both to Du Pont); idem, Pestic. Chem.: Hum. Welfare Environ., Proc. 5th Int. Congr. Pestic. 1, 243 (1983). Herbicidal activity and toxicity: R. H. Harding et al., Proc. West. Soc. Weed Sci. 34, 120 (1981). Mechanism of action: T. B. Ray, Proc. Br. Crop Prot. Conf. - Weeds 1985, 131. HPLC determn in soil and water: E. W. Zahnow, J. Agric. Food Chem. 33, 479 (1985). Degradation and bioaccumulation studies: J. Harvey et al., ibid. 590; J. J. Anderson, J. J. Dulka, ibid. 596. Field trials: R. L. Atkins et al., Proc. South. Weed Sci. Soc. 36, 300 (1983); in afforested areas: A. Nir, Z. Arenstein, Proc. Br. Crop Prot. Conf. - Weeds 1987, 787.

Zaldaride CAS Registry Number: 109826-26-8 1,3-二氢-1-[1-[(4-甲基-4H,6H-吡咯并[1,2-a][4,1]苯并氮杂-4-基)甲基]-4-哌啶]-2H-苯并咪唑-2-酮

CAS Name: 1,3-Dihydro-1-[1-[(4-methyl-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl)methyl]-4-piperidinyl]-2H-benzimidazol-2-one
Percent Composition: C 72.87%, H 6.59%, N 13.07%, O 7.47%
Literature References: Non-specific ion channel and calmodulin blocker. Prepn: J. W. F. Wasley, J. Norman, EP 233483; eidem, US 4758559 (1987, 1988 both to Ciba-Geigy). Synthesis: S. Boyer et al., J. Heterocycl. Chem. 25, 1003 (1988). Calmodulin inhibition: J. A. Norman et al., Mol. Pharmacol. 31, 535 (1987); and ion channel inhibition: R. Neuhaus, B. F. X. Reber, Eur. J. Pharmacol. 226, 183 (1992). Inhibition of gastric acid secretion: E. W. Black et al., J. Pharmacol. Exp. Ther. 248, 208 (1988); of secretory diarrhea in mice and rats: J. E. Shook et al., ibid. 251, 247 (1989). LC determn in human plasma: D. Chollet, M. Salanon, J. Chromatogr. 593, 73 (1992). Clinical trial in travelers' diarrhea: H. L. DuPont et al., Gastroenterology 104, 709 (1993).

Procodazole CAS Registry Number: 23249-97-0 丙考达唑

CAS Name: 1H-Benzimidazole-2-propanoic acid
Additional Names: b-(2-benzimidazolyl)propionic acid; 2-(2-carboxyethyl)benzimidazole; propazolTrademarks: Estimulocel (Alonga)
Percent Compositio...
Literature References: Non-specific, active immunoprotective agent against viral and bacterial infections. Prepn: J. Maier, Ann. 327, 17 (1903); R. Meyers, H. Lüders, ibid. 415, 29 (1918); B. Chatterjee, J. Chem. Soc. 1929, 2966; ES 407882 (1972 to Lafarquim). Pharmacological studies: C. Fernández et al., Rev. Clin. Esp. 135, 539 (1974); eidem, ibid. 141, 51 (1976). Clinical studies: M. Pérez Tascon, J. M. Monturio, Med. Klin. 181, 78 (1976).

Nilutamide CAS Registry Number: 63612-50-0 尼鲁米特

CAS Name: 5,5-Dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]-2,4-imidazolidinedione
Additional Names: 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4-dimethylimidazoline-2,5-dioneTrademarks: Anandron...
Literature References: Nonsteroidal antiandrogen. Prepn: J. Perronnet et al., DE 2649925; eidem, US 4097578 (1977, 1978 both to Roussel-UCLAF). Pharmacology: J.-P. Raynaud et al., J. Steroid Biochem. 11, 93 (1979). Review of kinetics, metabolism and clinical studies: idem et al., Prog. Clin. Biol. Res. 185A, 99-120 (1985); of therapeutic efficacy in prostate cancer: M. G. Harris et al., Drugs Aging 3, 9-25 (1993).

Toremifene CAS Registry Number: 89778-26-7 托瑞米芬

CAS Name: 2-[4-[(1Z)-4-Chloro-1,2-diphenyl-1-butenyl]phenoxy]-N,N-dimethylethanamine
Additional Names: (Z)-4-chloro-1,2-diphenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]phenyl]-1-butene
Percent Co...
Literature References: Nonsteroidal antiestrogen structurally similar to tamoxifen, q.v. Prepn: R. J. Toivola et al., EP 95875; eidem, US 4696949 (1983, 1987 both to Farmos). Pharmacology: S. Kallio et al., Cancer Chemother. Pharmacol. 17, 103 (1986). Antitumor effects in vitro and in vivo: L. Kangas et al., ibid. 109. HPLC determn in plasma: W. M. Holleran et al., Anal. Lett. 20, 871 (1987). Clinical evaluation in high-grade prostatic intraepithelial neoplasia: M. S. Steiner, C. R. Pound, Clin. Prostate Cancer 2, 24 (2003). Review of pharmacology and clinical efficacy in advanced breast cancer: L. R. Wiseman, K. L. Goa, Drugs 54, 141-160 (1997); in postmenopausal breast cancer: J. U. Mäenpää, S.-L. Ala-Fossi, Drugs Aging 11, 261-270 (1997).