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

Benidipine CAS Registry Number: 105979-17-7 贝尼地平

CAS Name: (4R)-rel-1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl (3R)-1-(phenylmethyl)-3-piperidinyl ester
Additional Names: (±)-(R*)-3-[(R*)-1-benzyl-3-p...
Literature References: Dihydropyridine calcium channel blocker. Prepn (stereochemistry unspecified): K. Muto et al., EP 63365; eidem, US 4448964 (1982, 1984 both to Kyowa). Prepn: eidem, EP 106275 (1984 to Kyowa); and toxicity data: eidem, Arzneim.-Forsch. 38, 1662 (1988). Structural studies: N. Hirayama, E. Shimizu, Acta Crystallogr. C47, 458 (1991). Series of articles on properties, pharmacology, determn and clinical evaluation: Arzneim.-Forsch. 38, 1666-1763 (1988). Review: H. Suzuki, T. Saruta, Cardiovasc. Drug Rev. 7, 25-38 (1989).

Barnidipine CAS Registry Number: 104713-75-9 (4S)-2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-3,5-二羧酸 (3S)-1-苄基-3-吡咯烷基-甲基酯

CAS Name: (4S)-1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl (3S)-1-(phenylmethyl)-3-pyrrolidinyl ester
Additional Names: (+)-(3'S,4S)-1-benzyl-3-pyrrolidinyl ...
Literature References: Dihydropyridine calcium channel blocker. Prepn (stereochemistry unspecified): T. Kojima, T. Takenaka, DE 2904552; eidem, US 4220649 (1979, 1980 both to Yamanouchi). Prepn and bioactivity of enantiomers: K. Tamazawa et al., J. Med. Chem. 29, 2504 (1986). GC-MS determn in plasma: T. Teramura et al., J. Chromatogr. 528, 191 (1990). Review of pharmacology and therapeutic efficacy: H. Satoh, Cardiovasc. Drug Rev. 9, 340-356 (1991).

Nifedipine CAS Registry Number: 21829-25-4 硝苯地平

CAS Name: 1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester
Additional Names: 4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbomethoxy-1,4-dihydropyridineTradema...
Literature References: Dihydropyridine calcium channel blocker. Prepn: Bossert, Vater, ZA 6801482; eidem, US 3485847 (1968, 1969 both to Bayer). Series of articles on pharmacology, pharmacokinetics, biotransformation, clinical studies: Arzneim.-Forsch. 22, 1-56, 330-388 (1972). Toxicity data: Vater et al., ibid. 1. Comprehensive description: S. L. Ali, Anal. Profiles Drug Subs. 18, 221-288 (1989). Review of analytical methods in biological fluids: P. A. Soons et al., J. Pharm. Biomed. Anal. 9, 475-484 (1991). Review of clinical efficacy in hypertension and Raynaud's phenomenon: W. Kiowski et al., Cardiovasc. Drugs Ther. 4, 935-940 (1990); in hypertension and angina: J. G. Tijssen, P. G. Hugenholtz, Eur. Heart J. 17, 1152-1157 (1996). Comparative clinical trial in prevention of complications from hypertension: M. J. Brown et al., Lancet 356, 366 (2000).

Elgodipine CAS Registry Number: 119413-55-7 依高地平

CAS Name: 4-(1,3-Benzodioxol-4-yl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid 2-[[(4-fluorophenyl)methyl]methylamino]ethyl 1-methylethyl ester
Additional Names: 2-[(p-fluorobenzyl)m...
Literature References: Dihydropyridine calcium channel blocker. Prepn: C. F. Torija, J. A. Galiano Ramos, EP 302980; eidem, US 4952592 (1989, 1990 both to Inst. Invest. Desarr. Quimicobiol.). In vitro and in vivo cardiovascular effects: J. Tamargo et al., Arzneim.-Forsch. 41, 895 (1991). Hemodynamic profile: C. Drieu la Rochelle et al., Br. J. Pharmacol. 111, 49 (1994). Clinical evaluation in coronary artery disease: H. Suryapranata et al., Am. J. Cardiol. 69, 1171 (1992). Clinical evaluation in chronic stable angina: D. U. Acharya et al., Eur. Heart J. 15, 665 (1994).

Lacidipine CAS Registry Number: 103890-78-4 拉西地平

CAS Name: (E)-4-[2-[3-(1,1-Dimethylethoxy)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid diethyl ester
Additional Names: diethyl (E)-4-[2-[2-(tert-butoxycarbon...
Literature References: Dihydropyridine calcium channel blocker. Prepn: C. Semeraro et al., DE 3529997; eidem, US 4801599 (1986, 1989 both to Glaxo). Clinical pharmacology: M. Safar et al., Clin. Pharmacol. Ther. 46, 94 (1989). HPTLC determn in urine: V. R. Kharat et al., J. Pharm. Biomed. Anal. 28, 789 (2002). Clinical trial in atherosclerosis: A. Zanchetti et al., Circulation 106, 2422 (2002). Review of use in hypertension: P. L. McCormack, A. J. Wagstaff, Drugs 63, 2327-2356 (2003).

Lercanidipine CAS Registry Number: 100427-26-7 乐卡地平

CAS Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-[(3,3-diphenylpropyl)methylamino]-1,1-dimethylethyl methyl ester
Additional Names: methyl 1,1,N-trimethyl-N-...
Literature References: Dihydropyridine calcium channel blocker. Prepn: D. Nardi et al., EP 153016; eidem, US 4705797 (1985, 1987 both to Recordati). Pharmacology: G. Bianchi et al., Pharmacol. Res. 21, 193 (1989). Clinical evaluation in hypertension: E. Rimoldi et al., Acta Ther. 20, 23 (1994).

Nisoldipine CAS Registry Number: 63675-72-9 尼索地平

CAS Name: 1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 2-methylpropyl ester
Additional Names: isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-p...
Literature References: Dihydropyridine calcium channel blocker. Prepn: E. Wehinger et al., DE 2549568; eidem, US 4154839 (1977, 1979 both to Bayer). Pharmacology: S. Kazda et al., Arzneim.-Forsch. 30, 2144 (1980). Hemodynamics: A. Vogt et al., ibid. 2162. Series of articles on pharmacokinetics: ibid. 38, 1093-1110 (1988). Reviews of pharmacology and clinical efficacy: H. A. Friedel, E. M. Sorkin, Drugs 36, 682-731 (1988); J. Mitchell et al., J. Clin. Pharmacol. 33, 46-52 (1993).

Nitrendipine CAS Registry Number: 39562-70-4 尼群地平

CAS Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid ethyl methyl ester
Additional Names: ethyl 1,4-dihydro-5-(acetoxycarbonyl)-2,6-dimethyl-4-(3-nitrophenyl)-3-py...
Literature References: Dihydropyridine calcium channel blocker. Prepn: H. Meyer et al., DE 2117571; eidem, US 3799934 (1972, 1974 both to Bayer); eidem, Arzneim.-Forsch. 31, 407 (1981). Series of articles on pharmacology: ibid. 2056-2067. Hemodynamic effects: H. O. Ventura et al., Am. J. Cardiol. 51, 783 (1983). Pharmacokinetics: L. Hansson et al., Hypertension 5, Suppl. II, II-25 (1983). HPLC determn in human serum: R. A. Janis et al., J. Clin. Pharmacol. 23, 266 (1983). Double-blind, controlled clinical trial: U. Brugmann et al., Herz 10, 53 (1985). Symposium on pharmacology and clinical efficacy: J. Cardiovasc. Pharmacol. 6 Suppl. 7, S929-S1113 (1984). Toxicology studies: K. Hoffmann, "Toxicological Studies with Nitrendipine" in Nitrendipine, A. Scriabine et al., Eds. (Urban Schwarzenberg, Baltimore, 1984) pp 25-32. Review: A. Scriabine et al., "Nitrendipine" in New Drugs Annual: Cardiovascular Drugs Vol. 2, A. Scriabine, Ed. (Raven Press, New York, 1984) pp 37-49.

Nimodipine CAS Registry Number: 66085-59-4 尼莫地平

CAS Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl 1-methylethyl ester
Additional Names: 2-methoxyethyl 1,4-dihydro-5-(isopropoxycarbonyl)-2,6-dim...
Literature References: Dihydropyridine calcium channel blocker. Prepn: H. Meyer et al., DE 2117571; eidem, US 3799934 (1972, 1974 to Bayer). Pharmacology: R. Towart, S. Kazda, Br. J. Pharmacol. 67, 409P (1979); K. Tanaka et al., Arzneim.-Forsch. 30, 1494 (1980); L. M. Auer, ibid. 31, 1423 (1981). Prepn of isomers and pharmacological comparison with racemate: R. Towart et al., ibid. 32, 338 (1982). Use as cerebral vasodilator: H. Meyer et al., GB 2018134; eidem, US 4406906 (1979, 1983 to Bayer). Effect on associative learning in aging rabbits: R. A. Deyo et al., Science 243, 809 (1989). GC and LC determns in biological fluids: G. J. Krol et al., J. Chromatogr. 305, 105 (1984). Clinical trial in prophylaxis of cerebral vasospasm: G. S. Allen et al., N. Engl. J. Med. 308, 619 (1983). Toxicology: H. Schlüter, Arzneim.-Forsch. 36, 1733 (1986). Series of articles on clinical pharmacology and therapeutic use: Am. J. Cardiol. 55(3), 139B-153B (1985).

Efonidipine CAS Registry Number: 111011-63-3 依福地平

CAS Name: 5-(5,5-Dimethyl-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylic acid 2-[phenyl(phenylmethyl)amino]ethyl ester, P-oxide
Additional Names: ...
Literature References: Dihydropyridine calcium channel blocker. Prepn: K. Seto et al., WO 8704439; idem et al., US 4885284 (1987, 1989 both to Nissan); and crystal structure: R. Sakoda et al., Chem. Pharm. Bull. 40, 2362 (1992). Stereoselective synthesis of enantiomers and crystal structure of (S)-form: idem et al., ibid. 2377. Pharmacology: C. Shudo et al., J. Pharm. Pharmacol. 45, 525 (1993). Mechanism of action study: T. Yamashita et al., Jpn. J. Pharmacol. 57, 337 (1991). Clinical study: T. Saito et al., Curr. Ther. Res. 52, 113 (1992).