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

Cloranolol CAS Registry Number: 39563-28-5 氯拉洛尔

CAS Name: 1-(2,5-Dichlorophenoxy)-3-[(1,1-dimethylethyl)amino]-2-propanol
Additional Names: 1-(tert-butylamino)-3-(2,5-dichlorophenoxy)-2-propanol
Percent Composition: C 53.44%, H 6.55%, Cl ...
Literature References: b-Adrenergic blocker. Prepn: G. Richter, DE 2213044 (1972 to Res. Inst. Pharm. Chem. Hungary), C.A. 78, 15780p (1973). Effect on plasma renin and blood pressure: I. Tenyi, Curr. Ther. Res. 21, 823 (1977). Pharmacology: M. I. K. Fekete et al., Arch. Int. Pharmacodyn. 248, 190 (1980). Electrophysiological characteristics: F. Solti, E. Czako, Int. J. Clin. Pharmacol. Ther. Toxicol. 18, 229 (1980). Clinical-pharmacological evaluation: E. Török et al., ibid. 200. GC-MS determn in plasma: E. Tomori, E. Elekes, J. Chromatogr. 204, 355 (1981). Multicenter clinical trial: E. Török et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 23, 650 (1985).

Butofilolol CAS Registry Number: 64552-17-6 丁菲洛尔

CAS Name: 1-[2-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-5-fluorophenyl]-1-butanone
Additional Names: (±)-5-fluoro-2-(2-hydroxy-3-t-butylaminopropoxy)butyrophenone; (±)-2'-[3-(t...
Literature References: b-Adrenergic blocker. Prepn: H. Demarne le Florence, DE 2528147; idem, US 4302601 (1976, 1981 both to C. M. Industries). Pharmacological study: G. G. Re et al., Boll. Soc. Ital. Biol. Sper. 56, 1264 (1980), C.A. 93, 197668y (1980). GC and HPLC determn in plasma and urine: J. P. Jeanniot et al., J. Chromatogr. 278, 301 (1983). Pharmacokinetics in humans: G. Houin et al., Int. J. Clin. Pharmacol. Res. 4, 175 (1984).

Tilisolol CAS Registry Number: 85136-71-6 替利洛尔

CAS Name: 4-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-2-methyl-1(2H)-isoquinolinone
Additional Names: 4-[3-(tert-butylamino)-2-hydroxypropoxy]-N-methylisocarbostyril
Percent Compositio...
Literature References: b-Adrenergic blocker. Prepn: H. Fukushima, Y. Suzuki, DE 2631080; eidem, US 4129565 (1977, 1978 both to Nisshin). Antiarrhythmic activity: K. Hashimoto et al., J. Pharmacol. Exp. Ther. 223, 801 (1982); and pharmacological profile: Y. Nakagawa et al., Arzneim.-Forsch. 34, 194 (1984). Receptor binding study: T. Nagatomo et al., Jpn. J. Pharmacol. 34, 249 (1984). Vasodilating activity in humans: T. Imaizumi et al., Arzneim.-Forsch. 38, 1342 (1988). HPLC determn in plasma: K. Yonezawa et al., J. Chromatogr. 339, 219 (1985). Toxicity data: S. Kawase et al., Oyo Yakuri 34, 499 (1987), C.A. 108, 161293m (1988).

Bunitrolol CAS Registry Number: 34915-68-9 布诺洛尔

CAS Name: 2-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]benzonitrile
Additional Names: o-[3-(tert-butylamino)-2-hydroxypropoxy]benzonitrile; 1-(2-cyanophenoxy)-2-hydroxy-3-tert-butylaminopro...
Literature References: b-Adrenergic blocker. Prepn: H. Koeppe et al., ZA 6803783; eidem, US 3541130 (1968, 1970 both to Boehringer, Ing.). Pharmacology: T. Kimura, Experientia 28, 813 (1972). Studies on absorption, distribution, metabolism, excretion in rats and mice: T. Suzuki, T. Rikihisa, Arzneim.-Forsch. 29, 1707 (1979). Clinical studies: A. Reale et al., J. Int. Med. Res. 4, 338 (1976); J. J. C. Jonker et al., Arzneim.-Forsch. 31, 1140 (1981). Toxicology study: M. Kanda et al., Oyo Yakuri 9, 457, 465, 499 (1975), C.A. 83, 172616 (1975).

Carazolol CAS Registry Number: 57775-29-8 咔唑心安

CAS Name: 1-(9H-Carbazol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanolTrademarks: Conducton (Klinge); Suacron (Praemix)
Percent Composition: C 72.46%, H 7.43%, N 9.39%, O 10.72%
Literature References: b-Adrenergic blocker. Prepn: H. Leinert et al., DE 2240599 (1974 to Boehringer, Mann.), C.A. 80, 133455a (1974). Comparative study of cardiac action: W. Bartsch et al., Arzneim.-Forsch. 27, 1022 (1977). Initial clinico-pharmacological study: E. Chorianopoulos et al., Herz/Kreislauf 9, 965 (1977), C.A. 88, 164460t (1978). Receptor binding studies: G. Kaiser et al., Arch. Pharmacol. 305, 41 (1978); R. B. Innis et al., Life Sci. 24, 2255 (1979). Use in treatment of stress syndrome in pigs: G. Ballarini, F. Guizzardi, Tieraerztl. Umsch. 36, 171 (1981).

Penbutolol CAS Registry Number: 38363-40-5 喷布洛尔

CAS Name: (2S)-1-(2-Cyclopentylphenoxy)-3-[(1,1-dimethylethyl)amino]-2-propanol
Additional Names: (S)-1-(tert-butylamino)-3-(o-cyclopentylphenoxy)-2-propanol; (-)-1-tert-butylamino-2-hydroxy-3-...
Literature References: b-Adrenergic blocker. Prepn: H. Ruschig et al., ZA 6807915; eidem, US 3551493 (1969, 1970 both to Hoechst). Preliminary chemistry and pharmacology: G. Härtfelder et al., Arzneim.-Forsch. 22, 930 (1972). Physicochemical and analytical study: P. Hajdu, D. Damm, ibid. 29, 602 (1979). Pharmacology: J. Kaiser et al., ibid. 30, 420 (1980). Action specificity: J. Kaiser ibid. 427. Crystallographic study: J. M. Leger et al., Mol. Pharmacol. 17, 339 (1980). Hemodynamic effects: P. Lund-Johansen, Eur. J. Clin. Pharmacol. 16, 149 (1979). Clinical study in hypertension: J. L. Cangiano et al., J. Clin. Pharmacol. 19, 384 (1979). HPLC determn in plasma: R. K. Bhamra et al., Biomed. Chromatogr. 1, 140 (1986). Review of pharmacology and therapeutic efficacy: R. C. Heel et al., Drugs 22, 1-25 (1981).

Practolol CAS Registry Number: 6673-35-4 普拉洛尔

CAS Name: N-[4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]acetamide
Additional Names: 4'-[2-hydroxy-3-(isopropylamino)propoxy]acetanilide; 1-(4-acetamidophenoxy)-3-isopropylamino-2-propa...
Literature References: b-Adrenergic blocker. Prepn: Howe, Smith, NL 6512676; eidem, US 3408387 (1966, 1968, to I.C.I.). Synthesis of R(+)-form: Danilewicz, Kemp, J. Med. Chem. 16, 168 (1973). Pharmacological studies: Dunlop, Shanks, Br. J. Pharmacol. Chemother. 32, 201 (1968); Barrett, Postgrad. Med. J. Suppl. 47, 7 (1971). Metabolic studies: Scales, Cosgrove, J. Pharmacol. Exp. Ther. 175, 338 (1970).

Befunolol CAS Registry Number: 39552-01-7 苯呋洛尔

CAS Name: 1-[7-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]-2-benzofuranyl]ethanone
Additional Names: 7-[2-hydroxy-3-(isopropylamino)propoxy]-2-benzofuranyl methyl ketone; 2-acetyl-7-(2-hydroxy-...
Literature References: b-Adrenergic blocker. Prepn: K. Ito et al., DE 2223184; eidem, US 3853923 (1972, 1974 both to Kakenyaku Kako). Prepn and activity of optical isomers: J. Nakano et al., Chem. Pharm. Bull. 36, 1399 (1988). Determn of befunolol and metabolites in human plasma: K. Kawahara, T. Ofuji, J. Chromatogr. 168, 266 (1979). Absorption, distribution, excretion in rats: H. Kitagawa et al., Oyo Yakuri 17, 383, 393 (1979), C.A. 91, 13374w-5x (1979). General pharmacology: S. Masumoto et al., Iyakuhin Kenkyu 10, 741 (1979), C.A. 92, 88015s (1980). Pharmacodynamics: S. Harada et al., Arch. Int. Pharmacodyn. Ther. 252, 262 (1981).

Bupranolol CAS Registry Number: 14556-46-8 布拉洛尔

CAS Name: 1-(2-Chloro-5-methylphenoxy)-3-[(1,1-dimethylethyl)amino]-2-propanol
Additional Names: 1-(tert-butylamino)-3-[(6-chloro-m-tolyl)oxy]-2-propanol; 1-(6-chloro-3-methylphenoxy)-3-tert-bu...
Literature References: b-Adrenergic blocker. Prepn: Kunz et al., DE 1236523 (1967 to Sanol-Arzneimittel Dr. Schwarz), C.A. 67, 64046k (1967) and US 3309406 (1967). Pharmacology: Waterloh et al., Arzneim.-Forsch. 19, 153, 330, 1710 (1969); Pendleton et al., Arch. Int. Pharmacodyn. Ther. 187, 75 (1970); P. Montastruc et al., Arch. Farmacol. Toxicol. 3, 93 (1977).

Metipranolol CAS Registry Number: 22664-55-7 美替洛尔

CAS Name: 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]-2,3,6-trimethylphenol 1-acetate
Additional Names: 1-(4-hydroxy-2,3,5-trimethylphenoxy)-3-(isopropylamino)-2-propanol 4-acetate; methypran...
Literature References: b-Adrenergic blocker. Prepn: L. Blaha et al., CS 128471 (1968), C.A. 71, 3129a (1969). Pharmacology: W. Bartsch et al., Arzneim.-Forsch. 27, 1022 (1977). Plasma levels and pharmacodynamics in man: O. Mayer et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 18, 113 (1980). Metabolic effects: R. P. Faupel, R. Gotzen, Med. Klin. 74, 929 (1979). Comparative effect in hypertension: K. Hayduk et al., Therapiewoche 29, 7528, 7530 (1979). Review of pharmacology and clinical trials in glaucoma and ocular hypertension: P. E. Battershill, E. M. Sorkin, Drugs 36, 601-615 (1988). Comprehensive description: J. Dohnal et al., Anal. Profiles Drug Subs. 19, 367-396 (1990).