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

Ondansetron CAS Registry Number: 99614-02-5 昂丹司琼

CAS Name: 1,2,3,9-Tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one
Percent Composition: C 73.70%, H 6.53%, N 14.32%, O 5.45%
Literature References: Specific serotonin (5HT3) receptor antagonist. Prepn: I. H. Coates et al., EP 191562; eidem, US 4695578 (1986, 1987 both to Glaxo). Pharmacology: A. Butler et al., Br. J. Pharmacol. 94, 397 (1988). Clinical trials in cancer chemotherapy-induced nausea and vomiting: M. G. Kris et al., J. Clin. Oncol. 6, 659 (1988); L. Cubeddu et al., N. Engl. J. Med. 322, 810 (1990); M. Marty et al., ibid. 816. Clinical evaluation in treatment of bulimia: P. L. Faris et al., Lancet 355, 792 (2000); in early onset alcoholism: B. A. Johnson et al., J. Am. Med. Assoc. 284, 963 (2000). Review of pharmacology and therapeutic use: A. Markham, E. M. Sorkin, Drugs 45, 931-952 (1993); of clinical pharmacokinetics: K. H. Simpson, F. M. Hicks, J. Pharm. Pharmacol. 48, 774-781 (1996).

Tropisetron CAS Registry Number: 89565-68-4 托烷司琼

CAS Name: 1H-Indole-3-carboxylic acid (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
Additional Names: 3a-tropanyl-1H-indole-3-carboxylic acid ester; 1aH,5aH-tropan-3a-yl indole-3-carboxyl...
Literature References: Specific serotonin (5-HT3) receptor antagonist. Prepn: P. Donatsch et al., DE 3322574 (1983 to Sandoz); idem et al., US 4789673 (1988). Pharmacology: B. P. Richardson et al., Nature 316, 126 (1985); F. M. Williams et al., J. Cardiovasc. Pharmacol. 7, 550 (1985). Receptor binding studies: C. Waeber et al., Neuroscience 31, 393 (1989). Clinical pharmacokinetics: V. Fischer et al., Drug Metab. Dispos. 20, 603 (1992). Series of articles on antiemetic efficacy in chemotherapy and radiotherapy: Drugs 43, Suppl. 3, 6-39 (1992). Review of pharmacology: C. Seynaeve et al., Anti-Cancer Drugs 2, 343-355 (1991); and toxicology: K. Kutz, Ann. Oncol. 4, Suppl. 3, S15-S18 (1993).

Propyl Gallate CAS Registry Number: 121-79-9 没食子酸丙酯

CAS Name: 3,4,5-Trihydroxybenzoic acid propyl ester
Additional Names: n-propyl gallate; gallic acid propyl ester; PG
Trademarks: Progallin P (Nipa); Tenox PG (Eastman)
Percent Composition...
Literature References: Spectrophotometric determn: C. S. Sastry et al., Talanta 29, 917 (1982). Effects on survival of Saccharomyces cerevisiae: V. L. Eubanks, L. R. Beuchat, J. Food Prot. 46, 29 (1983). Antioxidant effectiveness: M. A. Augustin, S. K. Berry, J. Am. Oil Chem. Soc. 60, 105 (1983). Comprehensive review of biological effects and toxicology: J. Am. Coll. Toxicol. 4, 23-64 (1985).

PBN CAS Registry Number: 3376-24-7 N-叔丁基-α-苯基硝酮

CAS Name: 2-Methyl-N-(phenylmethylene)-2-propanamine N-oxide
Additional Names: benzylidene-tert-butylamine oxide; N-tert-butyl-a-phenylnitrone
Percent Composition: C 74.54%, H 8.53%, N 7.90%...
Literature References: Spin trapping agent for short-lived radicals in biological systems. Prepn: W. D. Emmons, J. Am. Chem. Soc. 79, 5739 (1957); R. W. Murray et al., J. Org. Chem. 61, 8099 (1996). Effects on ischemia in brain: J. W. Phillis, C. Clough-Helfman, Med. Sci. Res. 18, 403 (1990); K. Pahlmark, B. K. Siesjö, Acta Physiol. Scand. 157, 41 (1996). Review of chemical properties and biological applications: G. Chen et al. in The Oxygen Paradox, PBN and Its Applications in Biology, K. J. A. Davies, F. Ursini, Eds. (Cleup Press, Italy, 1995) pp. 789-800.

Sorbinil CAS Registry Number: 68367-52-2 索比尼尔

CAS Name: (4'S)-6-Fluoro-2,3-dihydrospiro[4H-1-benzopyran-4,4'-imidazolidine]-2',5'-dione
Additional Names: (+)-(4S)-6-fluorospiro[chroman-4,4'-imidazolidine]-2',5'-dionePercent Composition: C ...
Literature References: Spirohydantoin aldose reductase inhibitor. Prepn of racemate and resolution of isomers: R. Sarges, DE 2821966; idem, US 4130714 (both 1978 to Pfizer). Synthesis: R. Sarges et al., J. Org. Chem. 47, 4081 (1982); N. L. Dirlam et al., J. Org. Chem. 52, 3587 (1987). Absolute configuration: R. Sarges et al., J. Med. Chem. 28, 1716 (1985). Effect on polyol accumulation in diabetic rats: M. J. Peterson et al., Metabolism 28, Suppl. 1, 456 (1979). Pharmacokinetics in humans: G. Foulds et al., Clin. Pharmacol. Ther. 30, 693 (1981). HPLC determn in human lens and plasma: P. Lloyd, M. J. C. Crabbe, J. Chromatogr. 343, 402 (1985). Preliminary clinical trials in diabetic neuropathy: R. J. Young et al., Diabetes 32, 938 (1983); J. Jaspan et al., Lancet 2, 758 (1983). Symposium on pharmacology and clinical efficacy: Metabolism 35, Suppl 1, 1-121 (1986).

Spiroxamine CAS Registry Number: 118134-30-8 螺环菌胺

CAS Name: 8-(1,1-Dimethylethyl)-N-ethyl-N-propyl-1,4-dioxaspiro[4.5]decane-2-methamineTrademarks: Impulse (Bayer)
Percent Composition: C 72.67%, H 11.86%, N 4.71%, O 10.76%
Literature References: Spiroketalamine fungicide for use on cereal crops; inhibits ergosterol synthesis. Prepn: W. Kraemer et al., DE 3735555; eidem, US 4851405 (1988, 1989 both to Bayer). Mode of action and field trials: S. Dutzmann et al., Brighton Crop Prot. Conf. - Pests Dis. 1996, 47. Series of articles on chemistry, activity, determn and ecobiology: Pflanzenschutz-Nachr. 50, 5-98 (1997).

Liranaftate CAS Registry Number: 88678-31-3 利拉萘酯

CAS Name: (6-Methoxy-2-pyridinyl)methylcarbamothioic acid O-(5,6,7,8-tetrahydro-2-naphthalenyl) ester
Additional Names: O-5,6,7,8-tetrahydro-2-naphthyl N-(6-methoxy-2-pyridyl)-N-methylthiocarba...
Literature References: Squalene epoxidase inhibitor. Prepn: BE 897021; T. Takematsu et al., US 4554012 (1983, 1985 both to Toyo Soda Manufacturing Co., Ltd.). Mode of action study: T. Morita et al., J. Med. Vet. Mycol. 27, 17 (1989). Antifungal spectrum: K. Iwata et al., Antimicrob. Agents Chemother. 33, 2118 (1989). Physicochemical properties and stability: H. Awano et al., Iyakuhin Kenkyu 23, 558 (1992).

TEMPO CAS Registry Number: 2564-83-2 2,2,6,6-四甲基哌啶-1-氧自由基

CAS Name: 2,2,6,6-Tetramethyl-1-piperidinyloxy
Additional Names: 2,2,6,6-tetramethylpentamethylene nitroxide
Percent Composition: C 69.18%, H 11.61%, N 8.96%, O 10.24%
Literature References: Stable nitroxide free radical used as reversible capping agent in "living" free radical polymerizations and as catalyst for selective oxidation of alcohols. Prepn: E. G. Ruzantsev et al., Bull. Acad. Sci. USSR Div. Chem. Sci. 1962, 2152. Crystal structure: Z. Ciunik, J. Mol. Struct. 412, 27 (1997). Thermal stability: M. V. Ciriano et al., J. Am. Chem. Soc. 121, 6375 (1999). Effect of acids on reaction rates: M. V. Baldovi et al., Macromolecules 29, 5497 (1996). Use in oxidation of alcohols: M. Zhao et al., J. Org. Chem. 64, 2564 (1999); in production of aminyl radicals: W. Huang et al., J. Am. Chem. Soc. 121, 3939 (1999); in polymerization: L. I. Gabaston et al., Polymer 40, 4505 (1999).

Dibromantin CAS Registry Number: 77-48-5 二溴海因

CAS Name: 1,3-Dibromo-5,5-dimethyl-2,4-imidazolidinedione
Additional Names: 1,3-dibromo-5,5-dimethylhydantoin; DBH; DBDMH
Percent Composition: C 21.00%, H 2.12%, Br 55.89%, N 9.80%, O 11.19%
Literature References: Stable, efficient, and economic bromination reagent; alternative to bromine or NBS, q.q.v. Prepn: O. O. Orazi, J. Meseri, An. Asoc. Quim. Argent. 38, 5 (1950); I. Markish, O. Arrad, Ind. Eng. Chem. Res. 34, 2125 (1995). Analytical applications in determn of iodide, iodine values, propylthiouracil, and selenium sulfide: M. Hilp, S. Senjuk, J. Pharm. Biomed. Anal. 25, 363 (2001); idem, ibid. 28, 81, 303, 337 (2002). Use in aromatic bromination reactions: H. Eguchi et al., Bull. Chem. Soc. Jpn. 67, 1918 (1994); X. Herault et al., Org. Prep. Proced. Int. 27, 652 (1995); C. Chassaing et al., Tetrahedron Lett. 38, 4415 (1997); in oxidation of thiols: A. Khazaei et al., Synthesis 2004, 2959. Review of bromination chemistry: R. A. Reed, Chem. Prod. 23, 299-302 (1960); A. Alam, Synlett 2005, 2403-2404.

Chondrillasterol CAS Registry Number: 481-17-4

CAS Name: (3b,5a,22E,24R)-Stigmasta-7,22-dien-3-ol
Percent Composition: C 84.40%, H 11.72%, O 3.88%
Literature References: Stereoisomeric with a-spinasterol, q.v. Isolated from the green alga Scenedesmus obliquus (Turpin) Kuetz., Scenedesmaceae: Bergmann, Feeney, J. Org. Chem. 15, 812 (1950). Synthesis: W. Sucrow et al., Phytochemistry 15, 1533 (1976); M. Anastasia et al., J. Chem. Soc. Perkin Trans. 1 1981, 2561.