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

Indoleacetic Acid CAS Registry Number: 87-51-4 吲哚-3-乙酸

CAS Name: 1H-Indole-3-acetic acid
Additional Names: heteroauxin; IAA
Percent Composition: C 68.56%, H 5.18%, N 8.00%, O 18.27%
Literature References: Plant hormone; recognized as the principal auxin of higher plants. Prepd by the reaction of indole with potassium glycolate at 250°: Johnson, Crosby, J. Org. Chem. 28, 1246 (1963). From indole and chloroacetic acid: Shagalov et al., US 3320281 (1967). Reviews: Leopold in The Hormones vol. IV, G. Pincus et al., Eds. (Academic Press, New York, 1964) pp 1-66; Thimann in The Physiology of Plant Growth and Development, M. B. Wilkins, Ed. (McGraw-Hill, New York, 1969) pp 1-45.

Factor XIII CAS Registry Number: 9013-56-3 血液凝固因子XIII

CAS Name: Blood-coagulation factor XIII
Additional Names: fibrin-stabilizing factor; FSF; fibrinase; Laki-Lorand factor; LLF
Trademarks: Fibrogammin (Centeon)
Literature References: Plasma enzyme precursor which, when activated by thrombin in the presence of Ca2+, converts soluble fibrin, q.v. gel to a tough insoluble clot: Laki, Lorand, Science 108, 280 (1948); Lorand, Nature 166, 694 (1950). During the terminal stage of blood-clotting, factor XIII catalyzes the formation of cross-links in the fibrin gel by eliminating NH3 in the transamidation reaction in which the e-amino group of lysine from a fibrin molecule forms a peptide linkage with a glutaminyl residue from a nearby fibrin monomer: Lorand et al., Biochem. Biophys. Res. Commun. 25, 629 (1966); Fuller, Doolittle, ibid. 694. Trypsin, papain, and reptilase also activate factor XIII: Lorand et al., ibid. 31, 222 (1968). Structure contains two each of two types of soluble proteinaceous subunits called the a and b chains; mol wt of subunits each about 80,000: Schwartz et al., J. Biol. Chem. 248, 1395 (1973). Amino acid sequence studies: Holbrook et al., Biochem. J. 135, 901 (1973). Clinical studies: Cucuianu et al., Thromb. Diath. Haemorrh. 30, 480 (1973). Review: L. Lorand, Ann. N.Y. Acad. Sci. 202, 6-30 (1972); A. G. Loewy, ibid. 41-58; C. G. Curtis, L. Lorand, Haemostasis: Biochemistry, Physiology Pathology, D. Ogston, B. Bennett, Eds. (Wiley-Interscience, New York, 1977) pp 186-201; eidem, Methods Enzymol. 45B, 177-191 (1976).

Texanol Isobutyrate CAS Registry Number: 6846-50-0 2,2,4-三甲基-1,3-戊二醇二异丁酸酯

CAS Name: 2-Methylpropanoic acid 2,2-dimethyl-1-(1-methylethyl)-1,3-propanediyl ester
Additional Names: 2,2,4-trimethyl-1,3-pentanediol diisobutyrate
Trademarks: TXIB (Eastman Chemical)
P...
Literature References: Plasticizer for PVC and other resins. Prepn: U. Schwenk, A. Becker, Ann. 756, 162 (1972). GC determn in PVC plastisol formulations: W. P. Hayes et al., J. Chromatogr. 139, 395 (1977). Toxicology: B. D. Astill et al., Toxicol. Appl. Pharmacol. 22, 387 (1972). Technical data sheet: "Eastman TXIB Plasticizer" (Eastman Chemical Co., publication L-151K, April 1998) 18 pp.

Lexipafant CAS Registry Number: 139133-26-9 1,2-丙二醇,3-(2-乙氧基苯氧基)-,(S)-(9CI)

CAS Name: N-Methyl-N-[[4-[(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)methyl]phenyl]sulfonyl]-L-leucine ethyl ester
Additional Names: N-methyl-N-[[a-(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)-p-tolyl...
Literature References: Platelet activating factor (PAF) antagonist. Prepn: M. Whittaker, A. Miller, WO 9203422; eidem, US 5200412 (1992, 1993 both to British Bio-Technology). Structure-activity report: M. Whittaker et al., J. Lipid Mediators Cell Signalling 10, 151 (1994). Pharmacology: F. M. Abu-Zidan et al., Pharmacol. Toxicol. 78, 23 (1996). Clinical evaluation in acute pancreatitis: A. N. Kingsnorth et al., Br. J. Surg. 82, 1414 (1995).

Israpafant CAS Registry Number: 117279-73-9 伊拉帕泛

CAS Name: 4-(2-Chlorophenyl)-6,9-dimethyl-2-[2-[4-(2-methylpropyl)phenyl]ethyl]-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
Additional Names: (±)-4-(o-chlorophenyl)-2-(p-isobutylp...
Literature References: Platelet activating factor (PAF) antagonist. Prepn: T. Tahara et al., EP 268242; eidem, US 4820703 (1988, 1989 both to Yoshitomi). Pharmacology: M. Terasawa et al., Prostaglandins 40, 553 (1990). Receptor binding study: S. Takehara et al., ibid. 571. Clinical evaluation in asthma: S. Hozawa et al., Am. J. Respir. Crit. Care Med. 152, 1198 (1995).

Ticlopidine CAS Registry Number: 55142-85-3 噻氯匹啶

CAS Name: 5-[(2-Chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
Additional Names: 5-(o-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
Percent Composition: C 63.74%, H 5.3...
Literature References: Platelet aggregation inhibitor. Prepn: DE 2404308; A. R. J. Castaigne, US 4051141 (1974, 1977 both to Cent. Etudes Ind. Pharm.); E. Braye, US 4127580 (1978 to Parcor). Metabolism: P. Godard et al., Eur. J. Drug Metab. Pharmacokinet. 3, 67 (1978); eidem, ibid. 4, 133 (1979); A. Tuong et al., ibid. 6, 91 (1981). Mode of action: G. Leblondel, P. Allain, Biochem. Pharmacol. 27, 2099 (1978); J. R. O'Brien et al., Thromb. Res. 13, 245 (1978); J. J. Bruno, ibid. 1983, Suppl. 4, 59. Pharmacology: A. Akashi et al., Arzneim.-Forsch. 30, 409, 415 (1980). Clinical studies: J. J. Thebault et al., J. Int. Med. Res. 5, 405 (1977); C. Lecrubier et al., Therapie 32, 189 (1977); T. Katsumura et al., Angiology 33, 357 (1982). Review of pharmacodynamics, pharmacokinetics and therapeutic use: E. Saltiel, A. Ward, Drugs 34, 222-262 (1987). Comprehensive description: F. J. Al-Shammary, N. A. A. Mian, Anal. Profiles Drug Subs. Excip. 21, 573-609 (1992).

Indobufen CAS Registry Number: 63610-08-2 吲哚布芬

CAS Name: 4-(1,3-Dihydro-1-oxo-2H-isoindol-2-yl)-a-ethylbenzeneacetic acid
Additional Names: (±)-2-[p-(1-oxo-2-isoindolinyl)phenyl]butyric acid; 1-oxo-2-[p-[(a-ethyl)carboxymethyl]phenyl]i...
Literature References: Platelet aggregation inhibitor. Prepn: R. W. J. Carney, G. de Stevens, DE 2034240 (1971 to Ciba), C.A. 74, 12547p (1971); P. N. Giraldi et al., DE 2154525; eidem, US 4118504 (1972, 1978 both to Carlo Erba); G. Nannini et al., Arzneim.-Forsch. 23, 1090 (1973). Pharmacology: M. Bergameaschi et al., Pharmacol. Res. Commun. 16, 979 (1984). HPLC determn in plasma: E. Wahlin-Boll et al., Eur. J. Clin. Pharmacol. 20, 375 (1981). Review of clinical pharmacokinetics and efficacy in vascular disease: L. R. Wiseman et al., Drugs 44, 445-464 (1992); in atherothrombosis: N. Bhana, K. J. McClellan, Drugs Aging 18, 369-388 (2001).

Satigrel CAS Registry Number: 111753-73-2 沙替格雷

CAS Name: 4-Cyano-5,5-bis(4-methoxyphenyl)-4-pentenoic acidPercent Composition: C 71.20%, H 5.68%, N 4.15%, O 18.97%
Literature References: Platelet aggregation inhibitor; inhibits phosphodiesterases and cyclooxygenase-1. Prepn: Y. Yamagishi et al., EP 238973; eidem, US 4978767 (1987, 1990 both to Eisai). Pharmacology: T. Fujimori et al., Arzneim.-Forsch. 37, 1143 (1987); eidem, Cardiovasc. Drug Rev. 9, 264 (1991). Selectivity for cyclooxygenase and phosphodiesterase isoforms: N. Nagakura et al., Biol. Pharm. Bull. 19, 828 (1996). GC-MS determn in plasma: Y. Yamano et al., J. Chromatogr. 528, 199 (1990). Clinical trial to prevent transient ischemic attacks: S. Maruyama et al., Angiology 46, 999 (1995).

Xemilofiban CAS Registry Number: 149820-74-6 珍米洛非班

CAS Name: (3S)-3-[[4-[[4-(Aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoic acid ethyl ester
Additional Names: ethyl (3S)-3-[3-[(p-amidinophenyl)carbamoyl]propionamido]-4-pentyno...
Literature References: Platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Prodrug converted in vivo to the active acid form. Prepn: P. R. Bovy et al., WO 9307867; eidem, US 5344957 (1993, 1994 both to Monsanto; Searle); J. Cossy et al., Bioorg. Med. Chem. Lett. 7, 1699 (1997). Structure-activity study: J. A. Zablocki et al., J. Med. Chem. 38, 2378 (1995). Pharmacology: N. S. Nicholson et al., Circulation 91, 403 (1995). Clinical pharmacokinetics: D. J. Kereiakes et al., ibid. 94, 906 (1996). Clinical evaluation in unstable angina: C. Simpfendorfer et al., ibid. 96, 76 (1997).

a -Ketoglutaric Acid CAS Registry Number: 328-50-7 α-酮戊二酸

CAS Name: 2-Oxopentanedioic acid
Additional Names: 2-oxoglutaric acid; 2-oxo-1,5-pentanedioic acid
Percent Composition: C 41.10%, H 4.14%, O 54.75%
Literature References: Plays an important role in amino acid metabolism (transamination) see Severo Ochoa, "Enzymic Mechanisms in the Citric Acid Cycle" in Adv. Enzymol. 15, 183-270 (1954). Prepn: Friedman, Kosower, Org. Synth. coll. vol. III, 510 (1955); Bottorff, Moore, ibid. coll. vol. V, 687 (1973). Microbial synthesis using a strain of Pseudomonas: Lockwood et al., US 2443919 (1948); Berger, Witt, US 2841616 (1958).