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

Taltirelin CAS Registry Number: 103300-74-9 他替瑞林

CAS Name: N-[[(4S)-Hexahydro-1-methyl-2,6-dioxo-4-primidinyl]carbonyl]-L-histidyl-L-prolinamide
Additional Names: (S)-N-(1-methyl-4,5-dihydroorotyl)-L-histidyl-L-prolinamide
Percent Composit...
Literature References: Analog of thyrotropin releasing hormone TRH, q.v., with pronounced CNS activity. Prepn: H. Sugano et al., EP 168042; eidem, US 4665056 (1986, 1987 both to Tanabe Seiyaku): M. Suzuki et al., J. Med. Chem. 33, 2130 (1990). Radioimmunoassay determn in plasma and urine: S. Morikawa et al., J. Pharm. Biomed. Anal. 16, 1267 (1998). CNS pharmacology: M. Yamamura et al., Jpn. J. Pharmacol. 53, 451 (1990). Effect on motor neuron survival: Y. Iwasaki et al., Neurol. Res. 19, 613 (1997). Review of pharmacology, toxicology, and clinical trials: K. Kinoshita et al., CNS Drug Rev. 4, 25-41 (1998).

Clopidogrel CAS Registry Number: 113665-84-2 氯吡格雷

CAS Name: (aS)-a-(2-Chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid methyl ester
Additional Names: methyl (+)-(S)-a-(o-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acet...
Literature References: Analog of ticlopidine, q.v.; inhibits ADP-induced platelet aggregation. Prepn (unspec. stereochem.): D. Aubert et al., EP 99802; eidem, US 4529596 (1984, 1985 both to Sanofi). Prepn of (+)-form: A. Badorc, D. Fréhel, EP 281459; eidem, US 4847265 (1988, 1989 both to Sanofi). Clinical pharmacology and mechanism of action: D. C. B. Mills et al., Arterioscler. Thromb. 12, 430 (1992). Clinical trial vs aspirin for prevention of atherothrombotic events: CAPRIE Steering Committee, Lancet 348, 1329 (1996). Review of pharmacology and therapeutic potential: G. Feuerstein et al., Expert Opin. Invest. Drugs 4, 425-430 (1995); of use in secondary prevention in stroke: H.-C. Diener et al., Expert Opin. Pharmacother. 6, 755-764 (2005).

Tetroxoprim CAS Registry Number: 53808-87-0 四氧普林

CAS Name: 5-[[3,5-Dimethoxy-4-(2-methoxyethoxy)phenyl]methyl]-2,4-pyrimidinediamine
Additional Names: 2,4-diamino-5-[3,5-dimethoxy-4-(2-methoxyethoxy)benzyl]pyrimidinePercent Composition: C 57....
Literature References: Analog of trimethoprim, q.v. Prepn: W. Liebenow, J. Prikryl, FR 2221147; eidem, US 3992379 (1974, 1976 both to Heumann). Series of articles on tetroxoprim and other antibacterial folate inhibitors: J. Antimicrob. Chemother. 5, Suppl. B, 1-239 (1979); on synthesis of radioactive tetroxoprim, tissue distribution, kinetics, HPLC determn: Arzneim.-Forsch. 30, 307-319 (1980). Effect on bacterial growth kinetics: J. K. Seydel, E. Wempe, Chemotherapy 26, 361 (1980). In vitro activity of the tetroxoprim-sulfadiazine combination: H. Hahn, A. Kirov, Arzneim.-Forsch. 30, 1047 (1980).

Drotaverine CAS Registry Number: 14009-24-6 盐酸屈他维林

CAS Name: 1-[(3,4-Diethoxyphenyl)methylene]-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline
Additional Names: 1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline; isodihydroperp...
Literature References: Analogue of papaverine, q.v. Prepn: BE 621917 (1962 to Chinoin), C.A. 59, 8713g (1963). Synthesis: E. Koltai et al., J. Labelled Compd. Radiopharm. 16, 351 (1979). Crystal structure: Z. Böcksei et al., Acta Crystallogr. C51, 1587 (1995). Absorption study: P. Szentmiklosi, S. Marton, Pharmazie 38, 611 (1983). Platelet aggregation and hemorrheological effects: Z. Kapui et al., Thromb. Res. 66, 693 (1992). Clinical pharmacokinetics and bioavailability: O. O. Bolaji et al., Eur. J. Drug Metab. Pharmacokinet. 21, 217 (1996). HPLC determn in biological fluids: eidem, J. Chromatogr. 622, 93 (1993). Clinical evaluation: D. Vecsey, Ther. Hung. 32, 127 (1984). Clinical effects on fetal development: A. E. Czeizel, M. Rockenbauer, Prenatal Neonat. Med. 1, 137 (1996).

Arborescin CAS Registry Number: 6831-14-7 (4aS,7S,9aS,9bR)-1,4A,7-三甲基-5,6,6A,7,9A,9B-六氢-3H-环氧乙烷并[8,8A]薁并[4,5-b]呋喃-8(4aH)-酮

CAS Name: (3aR,4aS,6aS,7S,9aS,9bR)-5,6,6a,7,9a,9b-Hexahydro-1,4a,7-trimethyl-3H-oxireno[8,8a]azuleno[4,5-b]furan-8(4aH)-one
Additional Names: 1,10-epoxy-6b-hydroxy-1b,5b,7a-guiai-3-en-12-oic ac...
Literature References: Ancient Greek contraceptive. Isoln from Artemisia arborescens L. and Matricaria globifera (Thunb.) Druce, Compositae: Meisels, Weizmann, J. Am. Chem. Soc. 75, 3865 (1953); Cekan et al., Collect. Czech. Chem. Commun. 25, 2553 (1960). Structure: Bates et al., Tetrahedron Lett. 1963, 1127; M. Suchy et al., Collect. Czech. Chem. Commun. 29, 1829 (1964). Synthesis and revised structure: M. Ando et al., Chem. Lett. 1978, 727. Stereochemistry: M. Ando et al., J. Org. Chem. 47, 3909 (1982).

Tetrahydrogestrinone CAS Registry Number: 618903-56-3 (8S,13S,14S,17S)-13,17-二乙基-17-羟基-1,2,6,7,8,13,14,15,16,17-十氢-3H-环戊二烯并[a]菲-3-酮

CAS Name: (17a)-13-Ethyl-17-hydroxy-18,19-dinorpregna-4,9,11-trien-3-one
Additional Names: 18a-homo-pregna-4,9,11-trien-17b-ol-3-one; THG
Percent Composition: C 80.72%, H 9.03%, O 10.24%
Literature References: Androgen and progestin; hydrogenation product of gestrinone, q.v. Discovery, synthesis, LC/MS/MS and GC/MS determn in urine: D. H. Catlin et al., Rapid Commun. Mass Spectrom. 18, 1245 (2004). Hormonal properties: A. K. Death et al., J. Clin. Endocrinol. Metab. 89, 2498 (2004). In vitro metabolism study: J.-F. Lévesque et al., Anal. Chem. 77, 3164 (2005).

Osaterone CAS Registry Number: 105149-04-0 奥沙特隆

CAS Name: 6-Chloro-17-hydroxy-2-oxapregna-4,6-diene-3,20-dione
Percent Composition: C 65.84%, H 6.91%, Cl 9.72%, O 17.54%
Literature References: Androgen receptor antagonist. Prepn: K. Shibata et al., EP 193871; eidem, US 4785103 (1986, 1988 both to Teikoku Hormone); K. Shibata et al., Chem. Pharm. Bull. 40, 935 (1992). Pharmacology: M. Murakoshi et al., Acta Pathol. Jpn. 42, 151 (1992); T. Ichikawa et al., Endocr. J. 40, 425 (1993); M. Murakoshi et al., ibid. 479.

Anecortave Acetate CAS Registry Number: 7753-60-8 δ-9(11)-氢化可的松醋酸酯

CAS Name: 21-(Acetyloxy)-17-hydroxypregna-4,9(11)-diene-3,20-dione
Additional Names: D4,9(11)-pregnadien-17a,21-diol-3,20-dione-21-acetateTrademarks: Retaane (Alcon )
Percent Composition: C ...
Literature References: Angiostatic steroid. Prepn: J. Fried, E. F. Sabo, J. Am. Chem. Soc. 75, 2273 (1953); R. P. Graber et al., ibid. 4722; J. Fried, E. F. Sabo, ibid. 79, 1130 (1957). Angiostatic activity in vitro: L. G. McNatt et al., J. Ocul. Pharmacol. Ther. 15, 413 (1999); in vivo: D. BenEzra et al., Invest. Ophthalmol. Visual Sci. 38, 1954 (1997). Clinical study in age-related macular degeneration: J. S. Slakter et al., Ophthalmology 110, 2372 (2003). Review of pharmacology: A. F. Clark, Expert Opin. Invest. Drugs 6, 1867-1877 (1997); and clinical experience: S. A. Vinores, IDrugs 8, 327-334 (2005).

Benazepril CAS Registry Number: 86541-75-5 贝那普利

CAS Name: (3S)-3-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-2,3,4,5-tetrahydro-2-oxo-1H-1-benzazepine-1-acetic acid
Additional Names: (3S)-1-(carboxymethyl)-[[(1S)-1-(ethoxycarbonyl)-3-phe...
Literature References: Angiotensin converting enzyme (ACE) inhibitor. Hydrolyzed in vivo to the active diacid metabolite. Prepn: J. W. H. Watthey, EP 72352; idem, US 4410520 (both 1983 to Ciba-Geigy); J. W. H. Watthey et al., J. Med. Chem. 28, 1511 (1985). Clinical pharmacology: M. D. Schaller et al., Eur. J. Clin. Pharmacol. 28, 267 (1985). GC-MS determn in plasma and urine: A. Sioufi et al., J. Chromatogr. 434, 239 (1988). Pharmacokinetics of benazepril and benazeprilat: G. Kaiser et al., Biopharm. Drug Dispos. 10, 365 (1989). Multicenter clinical trial in hypertension: M. Moser et al., ibid. 49, 322 (1991); in congestive heart failure: H. T. Colfer et al., Am. J. Cardiol. 70, 354 (1992).

Trandolapril CAS Registry Number: 87679-37-6 群多普利

CAS Name: (2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic acid
Additional Names: (3aR,7aS)-1-[N-[1(S)-(ethoxycarbonyl)-3-phen...
Literature References: Angiotensin converting enzyme (ACE) inhibitor. Prepn: H. Urbach et al., EP 84164; eidem, US 4933361 (1983, 1990 both to Hoechst). Enzyme inhibition and pharmacology: N. L. Brown et al., Eur. J. Pharmacol. 148, 79 (1988). Clinical pharmacology: F. De Ponti et al., Eur. J. Clin. Pharmacol. 40, 149 (1991). Clinical trial in prevention of death after myocardial infarction: L. Kober et al., N. Engl. J. Med. 333, 1670 (1995). Series of articles on pharmacology and clinical trials: Am. J. Hypertens. 8, 63S-74S (1995). Clinical trial in diabetic neuropathy: R. A Malik et al., Lancet 352, 1978 (1998).