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

Ronifibrate CAS Registry Number: 42597-57-9 罗尼贝特

CAS Name: 3-Pyridinecarboxylic acid 3-[2-(4-chlorophenoxy)-2-methyl-1-oxopropoxy]propyl ester
Additional Names: 3-(nicotinoyloxy)propyl p-chlorophenoxyisobutyrate; 3-[a-(p-chlorophenoxy)isobuty...
Literature References: Diester of clofibric and nicotinic acids, q.q.v. Prepn: Y. Hirata et al., JP Kokai 73 40777 (1973 to Yamanouchi), C.A. 79, 66180w (1973); H. Shindo et al., JP Kokai 74 30377 (1974 to Kowa Pharm.), C.A. 81, 135984s (1974). Clinical trial in hyperdyslipidemia: A. Bucalossi et al., Clin. Ter. 89, 127 (1979). Efficacy and tolerability: G. Buzzelli et al., ibid. 251.

Dihydroisocodeine CAS Registry Number: 795-38-0 (-)-二氢异可待因

CAS Name: (5a,6b)-4,5-Epoxy-3-methoxy-17-methylmorphinan-6-ol
Additional Names: DHIC
Percent Composition: C 71.73%, H 7.69%, N 4.65%, O 15.93%
Literature References: Differs from dihydrocodeine only by the spatial arrangement of the -CHOH- group. Prepn by catalytic reduction of isocodeine: Speyer, Krauss, Ann. 432, 233 (1923); Lutz, Small, J. Am. Chem. Soc. 54, 4724 (1932); Rapoport, Payne, J. Org. Chem. 15, 1097 (1950); by epimerization of dihydrocodeine: Baizer, US 2774762 (1956 to N.Y. Quinine and Chem. Works).

Pyrocalciferol CAS Registry Number: 128-27-8 (3beta,10alpha,22E)-麦角甾-5,7,22-三烯-3-醇

CAS Name: (3b,10a,22E)-Ergosta-5,7,22-trien-3-ol
Additional Names: 9a-lumisterol; 9a-lumista-5,7,22-trien-3b-ol
Percent Composition: C 84.78%, H 11.18%, O 4.03%
Literature References: Differs from ergosterol in the steric configuration at C-9 and C-10. Formation via isopyrocalciferol: Askew et al., Proc. Roy. Soc. London B109, 488 (1932); Windaus et al., Nachr. Ges. Wiss. Goettingen Math.-Phys. Kl. 1932, 150. Dehydrogenation with selenium gives Diel's hydrocarbon (3¢-methyl-1,2-cyclopentenophenanthrene). Fieser, Fieser, Steroids (New York, 1959) pp 136-143, argue the configuration at C-9 and C-10. See also Castells et al., J. Chem. Soc. 1959, 1159. Critical examination and comparison with other unnatural steroids: Castells et al., ibid. 1962, 2907.

Isopyrocalciferol CAS Registry Number: 474-70-4 (3beta,9beta,22E)-麦角甾-5,7,22-三烯-3-醇

CAS Name: (3b,9b,22E)-9-Ergosta-5,7,22-trien-3-ol
Additional Names: 9b-ergosterol
Percent Composition: C 84.78%, H 11.18%, O 4.03%
Literature References: Differs sterically from pyrocalciferol at C-10, from ergosterol at C-9. See ref under Pyrocalciferol. Stereochemistry: Castells et al., J. Chem. Soc. 1959, 1159. Selenium dehydrogenation gives Diel's hydrocarbon (3¢-methyl-1,2-cylopentenophenanthrene).

Potassium Tetraiodocadmate CAS Registry Number: 584-10-1 碳三硫酸,二钾盐(9CI)

CAS Name: Dipotassium tetraiodocadmate(2-)
Additional Names: cadmium potassium iodide; potassium cadmium iodide; potassium iodocadmate; Marme's reagent
Percent Composition: Cd 16.10%, I 72.7...
Literature References: Dihydrate prepd from aq solns of stoichiometric amounts of CdI2 and KI; must be recrystallized from water at low temps: Croft, Philos. Mag. 21, 355 (1842); J. Prakt. Chem. 58, 399 (1856); Hittorf, Pogg. Ann. 106, 525 (1859); Eder, Photogr. Mitt. 13, 67 (1867); Rimbach, Ber. 38, 1562 (1905).

Edatrexate CAS Registry Number: 80576-83-6 依达曲沙

CAS Name: N-[4-[1-[(2,4-Diamino-6-pteridinyl)methyl]propyl]benzoyl]-L-glutamic acid
Additional Names: 10-ethyl-10-deazaaminopterin; 10-EdAM; 10-EDAAMPercent Composition: C 56.52%, H 5.39%, N 20...
Literature References: Dihydrofolate reductase inhibitor. Prepn: F. M. Sirotnak, J. I. DeGraw, FR 2464956 (1981 to SRI International); J. I. DeGraw, Jr., F. M. Sirotnak, US 4369319 (1983). Synthesis: J. I. DeGraw et al., J. Med. Chem. 25, 1227 (1982); and resolution of diastereomers: eidem, ibid. 29, 1056 (1986). HPLC determn: J. J. Kinahan et al., Anal. Biochem. 150, 203 (1985); O. Van Tellingen et al., J. Chromatogr. 529, 135 (1990). Pharmacology and toxicology: M. P. Fanucchi et al., Cancer Res. 47, 2334 (1987). Clinical evaluation in non-small cell lung cancer: J. S. Lee et al, Invest. New Drugs 8, 299 (1990). Review of pharmacology and antitumor activity: F. M. Sirotnak et al., NCI Monogr. 5, 127-131 (1987).

Pyrimethamine CAS Registry Number: 58-14-0 乙胺嘧啶

CAS Name: 5-(4-Chlorophenyl)-6-ethyl-2,4-pyrimidinediamine
Additional Names: 2,4-diamino-5-(p-chlorophenyl)-6-ethylpyrimidineTrademarks: Daraprim (GSK); Malocide (Aventis)
Percent Compositio...
Literature References: Dihydrofolate reductase inhibitor; generally used in combination with other antimicrobial agents. Prepn: P. B. Russell, G. H. Hitchings, J. Am. Chem. Soc. 73, 3763 (1951); G. H. Hitchings et al., US 2576939 (1951 to Burroughs Wellcome); W. Logemann et al., Ber. 87, 435 (1954); R. M. Jacob, US 2680740 (1954 to Rhône-Poulenc). Review of antimicrobial activity and mechanism of action: Burchall in Antibiotics vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (Springer-Verlag, New York, 1975) pp 312-320. Comprehensive description: M. A. Loutfy, H. Y. Aboul-Enein, Anal. Profiles Drug Subs. 12, 463-482 (1983). LC-MS determn in plasma: B. A. Sinnaeve et al., J. Chromatogr. A 1076, 97 (2005). Clinical evaluations in toxoplasmosis in AIDS patients: C. Leport et al., Am. J. Med. 84, 94 (1988); B. Dannemann et al., Ann. Intern. Med. 116, 33 (1992). Review of clinical experience in malaria: H. M. McIntosh et al., Ann. Trop. Med. Parasitol. 93, 265-270 (1998); C. V. Plowe et al., Br. Med. J. 328, 545 (2004).

Brodimoprim CAS Registry Number: 56518-41-3 溴莫普林

CAS Name: 5-[(4-Bromo-3,5-dimethoxyphenyl)methyl]-2,4-pyrimidinediamine
Additional Names: 2,4-diamino-5-(4-bromo-3,5-dimethoxybenzyl)pyrimidinePercent Composition: C 46.03%, H 4.46%, Br 23.56%,...
Literature References: Dihydrofolate reductase inhibitor; structural analog of trimethoprim, q.v. Prepn: M. Hoffer, I. Kompis, DE 2452889 (1975 to Hoffmann-La Roche), C.A. 83, 97361 (1975); I. Kompis, US 4024145 (1977 to Hoffmann-La Roche); I. Kompis, A. Wick, Helv. Chim. Acta 60, 3025 (1977). Antibacterial activity: G. Giammanco et al., Drugs Exp. Clin. Res. 9, 721 (1983). Comparison with trimethoprim as inhibitor of dihydrofolate reductase: R. L. Then et al., Rev. Infect. Dis. 4, 372 (1982); R. L. Then, F. Hermann, Chemotherapy (Basel) 30, 18 (1984). Antimycobacterial activity in vitro: J. K. Seydel et al., ibid. 29, 249 (1983). Pharmacokinetics in human serum, skin blister fluid: T. Kalager et al., Chemotherapy (Basel) 31, 405 (1985). Clinical evaluation in respiratory infections: H. A. Salmi et al., Drugs Exp. Clin. Res. 12, 349 (1986); in urinary tract infections: F. Scaglione et al., Int. J. Clin. Pharmacol. Res. 15, 121 (1995); in bacterial cystitis: E. V. Cosmi et al., Eur. J. Obstet. Gynecol. Reprod. Biol. 64, 207 (1996).

Sulfadoxine CAS Registry Number: 2447-57-6 磺胺多辛

CAS Name: 4-Amino-N-(5,6-dimethoxy-4-pyrimidinyl)benzenesulfonamide
Additional Names: N'-(5,6-dimethoxy-4-pyrimidinyl)sulfanilamide; 6-(4-aminobenzenesulfonamido)-4,5-dimethoxypyrimidine; 4-sul...
Literature References: Dihydropteroate synthetase inhibitor. Prepn: BE 618639; H. Bretschneider et al., US 3132139 (1962, 1964 both to Hoffmann-La Roche). Toxicological, chemotherapeutic and pharmacokinetic studies: E. Böhni et al., Chemotherapy 14, 195-226 (1969). Comprehensive description: V. K. Kapoor, Anal. Profiles Drug Subs. 17, 571-605 (1988). Enzyme inhibition in vitro: Y. Zhang, S. R. Meshnick, Antimicrob. Agents Chemother. 35, 267 (1991). Determn in plasma using supercritical fluid chromatography: S. I. Bhoir et al., J. Chromatogr. B 757, 39 (2001). Clinical trial of combination with pyrimethamine, q.v., for malaria: C. V. Plowe et al., Br. Med. J. 328, 545 (2004).

Felodipine CAS Registry Number: 72509-76-3 非洛地平

CAS Name: 4-(2,3-Dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl esterTrademarks: Agon (TheraPharm); Feloday (Novartis); Flodil (AstraZeneca); Hydac (Aventis); ...
Literature References: Dihydropyridine calcium channel blocker marketed as the racemate. Prepn: P. B. Berntsson et al., EP 7293; eidem, US 4264611 (1980, 1981 both to AB Hassle). Conformation: P. B. Berntsson, R. E. Carter, Acta Pharm. Suec. 18, 221 (1981). Interaction with calmodulin, q.v.: S. L. Boström et al., Nature 292, 777 (1981). Diuretic-natriuretic properties: G. F. Dibona et al., Clin. Res. 30, 571A (1982). Hemodynamic effects in coronary patients: P. Decoster et al., Eur. J. Clin. Invest. 12, 43 (1982). Enantioselective determn in plasma: P. A. Soons et al., J. Chromatogr. 528, 343 (1990); HPLC-MS-MS determn in plasma: L. H. Miglioranca et al., J. Chromatogr. B 814, 217 (2005). Pharmacokinetics and pharmacodynamics: B. Edgar et al., Biopharm. Drug Dispos. 8, 235 (1987). Pharmacokinetics, vascular selectivity, effects on hypertension, hemodynamics and renal function: Drugs 29, Suppl. 2, 1-212 (1985).