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

Sodium Glycerophosphate CAS Registry Number: 1334-74-3 二钠甘油磷酸酯

CAS Name: 1,2,3-Propanetriol mono(dihydrogen phosphate) disodium salt
Percent Composition: C 16.68%, H 3.27%, Na 21.28%, O 44.43%, P 14.34%
Literature References: Three isomers exist: The b-glycerophosphoric acid disodium salt ((HOCH2)2CHOPO3Na2) and D(+)- and L(-)-a-glycerophosphoric acid disodium salt (HOCH2CH(OH)CH2OPO3Na2). Prepn: H. King, F. L. Pyman, Pharm. J. 92, 511 (1914). Exptl use in diagnosis of prostatic carcinoma: M. K. Schwartz et al., Ann. N.Y. Acad. Sci. 166, 775 (1969). Chronic toxicity study of b-form: K. L. Raheja et al., Toxicology 8, 115 (1977). Efficacy of b-form as cariostatic agent: T. H. Grenby, J. M. Bull. Arch. Oral Biol. 20, 717 (1975). GC determn: Y. Handa et al., J. Chromatogr. 206, 387 (1981).

Benzil Dioxime CAS Registry Number: 23873-81-6 二联苯乙二醛肟

CAS Name: Diphenylethanedione dioxime
Additional Names: diphenylglyoxime
Percent Composition: C 69.99%, H 5.03%, N 11.66%, O 13.32%
Literature References: Three isomers occur: a or anti, b or syn, g or amphi. Prepn of a-form from benzil and hydroxylamine hydrochloride: Brady, Perry, J. Chem. Soc. 127, 2874 (1925); F. J. Welcher, Organic Analytical Reagents vol. III (Van Nostrand, New York, 1947) pp 224-227; Boyer et al., J. Am. Chem. Soc. 77, 5688 (1955). Prepn of b-form: Brady, Perry, loc. cit.; Boyer et al., loc. cit. Prepn of g-form: Welcher, loc. cit., pp 227-228; see also Boyer et al., loc. cit.

Dextranomer CAS Registry Number: 56087-11-7

CAS Name: Dextran 2,3-dihydroxypropyl 2-hydroxy-1,3-propanediyl ethers
Trademarks: Debrisan (Pharmacia); Debrisorb (Pharmacia)
Literature References: Three-dimensional hydrophilic network of a dextran polymer, linked by cross-chains of epichlorohydrin, q.v.; it absorbs moisture and small molecules from suppurating wounds. Chronic tissue response to implantation: J. Falk, G. Tollerz, Clin. Ther. 1(3), 185 (1977). Potential allergic contact sensitization in guinea pigs: G. Jonsson, ibid. 1(4), 260 (1978). Efficacy in treatment of ulcers and wounds: J. Soul, Br. J. Clin. Pract. 32, 172 (1978); P. N. Sawyer et al., Surgery 85, 201 (1979); S. Di Mascio, Am. J. Nurs. 79, 684 (1979). Review: R. C. Heel et al., Drugs 18, 89-102 (1979).

Batroxobin CAS Registry Number: 9039-61-6 丝氨酸蛋白酶,Bothrops atrox

CAS Name: Bothrops atrox serine proteinase
Additional Names: Bothrops venom proteinase
Trademarks: Botropase (Ravizza); Defibrase (Gerot)
Literature References: Thrombin-like enzyme from the venom of Bothrops atrox (Linn.), a pit viper found in several varieties in Southern and Central America. Prepn of conc extract from B. jararaca venom and coagulative properties: D. von Klobusitzky, Arch. Exp. Pathol. Pharmakol. 179, 204 (1935). The enzyme from B. atrox venom is hemostatic at low doses and acts as a blood anti-coagulant at higher doses. Composition and manuf: E. E. Percs et al., DE 2201993; eidem, US 3849252 (1972, 1974 both to Pentapharm). Studies on the subunit structure of fibrin produced by batroxobin: P. Mattock, M. P. Esnouf, Nature New Biol. 233, 277 (1971). In vitro blood-clotting activity: K. O. Wik et al., Br. J. Haematol. 23, 37 (1972). Electron microscopic study: S. Ishimaru et al., Thromb. Haemostasis 45, 276 (1981). Clinical pharmacology: K. Fukutake et al., Nippon Ketsueki Gakkai Zasshi 44, 1178 (1981), C.A. 96, 62775x (1982). Review of characterization, properties: K. G. Stocker, G. H. Barlow, Aktuel. Probl. Angiol. 26, 45-62 (1975).

Isbogrel CAS Registry Number: 89667-40-3 伊波格雷

CAS Name: (E)-7-Phenyl-7-(3-pyridinyl)-6-heptenoic acidPercent Composition: C 76.84%, H 6.81%, N 4.98%, O 11.37%
Literature References: Thromboxane A2 (TXA2) synthetase inhibitor. Prepn: S. Terao, K. Nishikawa, EP 98690; eidem, US 4518602 (1984, 1985 both to Takeda); and inhibition of TXA2: K. Kato et al., J. Med. Chem. 28, 287 (1985). Pharmacology: Z. Terashita et al., Thromb. Res. 41, 223 (1986). Antithrombotic effect in experimental thrombi: T. Matsubara et al., Am. Heart J. 118, 837 (1989). Clinical pharmacokinetics: T. Kuzuya et al., Cardiovasc. Drugs Ther. 2, 693 (1988). Clinical trial: R. Hattori et al., Jpn. Circ. J. 55, 324 (1991).

Ramatroban CAS Registry Number: 116649-85-5 雷马曲班

CAS Name: (3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid
Additional Names: (+)-(3R)-3-(p-fluorobenzenesulfonamido)-1,2,3,4-tetrahydrocarbazole-9-propi...
Literature References: Thromboxane A2 receptor antagonist. Prepn: H. Böshagen et al., DE 3631824; eidem, US 4965258 (1988, 1990 both to Bayer); and absolute configuration: U. Rosentreter et al., Arzneim.-Forsch. 39, 1519 (1989). Series of articles on pharmacology: ibid. 1522-1530. Clinical evaluation in asthma: H. Aizawa et al., Chest 109, 338 (1996).

Domitroban CAS Registry Number: 112966-96-8 多米曲班

CAS Name: (5Z)-7-[(1R,2S,3S,4S)-3-[(Phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-yl]-5-heptenoic acid
Additional Names: (+)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]-5-hep...
Literature References: Thromboxane A2-receptor antagonist. Prepn of (±)-form: F. Watanabe et al., EP 226346; eidem, US 4861913 (1987, 1989 both to Shionogi); and isomers: M. Narisada et al., J. Med. Chem. 31, 1847 (1988). Prepn of (+)-form: M. J. Martinelli, J. Org. Chem. 55, 5065 (1990); M. Ohtani et al., ibid. 56, 2122 (1991). Pharmacology: A. Arimura et al., Int. Arch. Allergy Immunol. 98, 239 (1992). GC determn in plasma: J. Okamoto et al., J. Chromatogr. 583, 45 (1992); in urine: eidem, ibid. 53. Clinical pharmacokinetics: A. Fujimura et al., J. Clin. Pharmacol. 36, 409 (1996). Clinical evaluation in asthma: M. Fujimura et al., Pulm. Pharmacol. 8, 251 (1995).

Seratrodast CAS Registry Number: 112665-43-7 塞曲司特

CAS Name: z-(2,4,5-Trimethyl-3,6-dioxo-1,4-cyclohexadien-1-yl)benzeneheptanoic acid
Additional Names: (±)-7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7-phenylheptanoic acidTrademarks: Bronica...
Literature References: Thromboxane A2-receptor antagonist. Prepn: S. Terao, Y. Maki, EP 171251; eidem, US 5180742 (1986, 1993 both to Takeda); M. Shiraishi et al., J. Med. Chem. 32, 2214 (1989). Effect on thromboxane A2/prostaglandin endoperoxidase-receptor: Y. Imura et al., Jpn. J. Pharmacol. 52, 35 (1990). Clinical effect in asthma: M. Fujimura et al., J. Allergy Clin. Immunol. 87, 23 (1991). Clinical pharmacokinetics: Z. Hussein et al., Clin. Pharmacol. Ther. 55, 441 (1994).

Broxuridine CAS Registry Number: 59-14-3 5-溴-2'-脱氧尿苷

CAS Name: 5-Bromo-2'-deoxyuridine
Additional Names: 5-bromouracil deoxyriboside; BrdUrd; BUdRTrademarks: Broxine (NeoPharm); Neomark (NeoPharm); Radibud (Takeda)
Percent Composition: C 35.20...
Literature References: Thymidine, q.v., analog. Preferentially incorporated into cellular DNA in place of thymidine during replication causing increased radiosensitivity of the cell. Prepn and inhibition of DNA biosynthesis: R. E. Beltz, D. W. Visser, J. Am. Chem. Soc. 77, 736 (1955); T. J. Bardos et al., ibid. 4279. X-ray crystallography: J. Iball et al., Nature 209, 1230 (1966). HPLC determn in plasma: D. A. Ganes, J. G. Wagner, J. Chromatogr. 432, 233 (1988). Clinical studies in brain tumors: H. S. Greenberg et al., Neurology 44, 1715 (1994); T. L. Phillips et al., Int. J. Radiat. Oncol. Biol. Phys. 21, 709 (1991). Review of radiobiology and therapeutic potential: T. J. Kinsella et al., ibid. 10, 1399-1406 (1984); of genetic toxicology: S. M. Morris, Mutat. Res. 258, 161-188 (1991); of role in management of CNS tumors: A. Freese et al., J. Neuro-Oncol. 20, 81-95 (1994). Series of reviews on diagnostic and research use: F. Dolbeare, Histochem. J. 27, 339-369, 923-964 (1995); 28, 531-575 (1996).

Thyropropic Acid CAS Registry Number: 51-26-3 去氨甲碘安

CAS Name: 4-(4-Hydroxy-3-iodophenoxy)-3,5-diiodohydrocinnamic acid
Additional Names: 3,3',5-triiodothyropropionic acid; b-[4-(3'-iodo-4'-hydroxyphenoxy)-3,5-diiodophenyl]propionic acid
Trade...
Literature References: Thyroid hormone analog. Prepd by iodination of 3,5-diiodothyropropionic acid: Tomita, Lardy, J. Biol. Chem. 219, 595 (1956).