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

Pioglitazone CAS Registry Number: 111025-46-8 匹格列酮

CAS Name: 5-[[4-[2-(5-Ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione
Additional Names: (±)-5-[p-[2-(ethyl-2-pyridyl)ethoxy]benzyl]-2,4-thiazolidinedionePercent Composition: ...
Literature References: Insulin sensitizer. Prepn: K. Meguro, T. Fujita, EP 193256; eidem, US 4687777 (1986, 1987 both to Takeda); T. Sohda et al., Arzneim.-Forsch. 40, 37 (1990). Pharmacology: H. Ikeda et al., ibid. 156. HPLC determn in serum: W. Z. Zhong, D. B. Lakings, J. Chromatogr. 490, 377 (1989). Mechanism of action: C. Hofmann et al., Endocrinology 129, 1915 (1991); M. Kobayashi et al., Diabetes 41, 476 (1992). Effect on adipocyte differentiation: T. Sandouk et al., Am. J. Physiol. 264, C1600 (1993). Clinical evaluation in noninsulin-dependent diabetes: R. Kawamori et al., Diabetes Res. Clin. Pract. 41, 35 (1998).

Rosiglitazone CAS Registry Number: 122320-73-4 罗格列酮

CAS Name: 5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione
Additional Names: 5-[4-[2-[N-methyl-N-(2-pyridinyl)amino]ethoxy]benzyl]-2,4-thiazolidinedionePercent Comp...
Literature References: Insulin sensitizer; binds to peroxisome proliferator activated receptor gamma (PPAR-g). Prepn: R. M. Hindley, EP 306228; idem, US 5002953 (1989, 1991 both to Beecham); B. C. C. Cantello et al., J. Med. Chem. 37, 3977 (1994). Pharmacology: N. D. Oakes et al., Diabetes 43, 1203 (1994). Binding study: D. E. Mais et al., Med. Chem. Res. 7, 325 (1997). Clinical pharmacokinetics and bioavailability: M. I. Freed et al., Eur. J. Clin. Pharmacol. 55, 53 (1999). Review of pharmacology and clinical experience: J. A. Barman Balfour, G. L. Plosker, Drugs 57, 921-930 (1999).

Ceruloplasmin CAS Registry Number: 9031-37-2 血浆铜蓝蛋白来自人血清

Additional Names: Caeruloplasmin; ferroxidase
Literature References: Intensely blue colored copper-containing glycoprotein of the a2-globulin fraction of mammalian blood; it is the principal copper transport protein and is believed to play an important role in iron mobilization via its ferroxidase activity. First reported by C. G. Holmberg, Acta Physiol. Scand. 8, 227 (1944). Isoln, purification and description of properties of porcine and human ceruloplasmin: C. G. Holmberg, C. B. Laurell, Acta Chem. Scand. 2, 550 (1948). Ceruloplasmin accounts for 90-95% of the circulating copper in normal mammals. Its concentration increases by a factor of 2 to 3 during pregnancy and varies significantly in several diseases and hormonal conditions. Prepd by Cohn cold ethanol fractionation: Cohn et al., J. Am. Chem. Soc. 68, 459 (1946); Steinbuch, Quentin, Nature 183, 323 (1959); and further purified from fraction IV: Sanders et al., Arch. Biochem. Biophys. 84, 60 (1959); US 3003918 (1961 to Merck Co.). Different mol wts have been reported for human ceruloplasmin, ranging from 126,000 to 160,000; the most generally accepted is 134,000 ±3000, cf. L. Ryder, I. Björk, Biochemistry 15, 3411 (1976). Chemical and structural studies of porcine ceruloplasmin: Osaki et al., J. Biochem. (Tokyo) 48, 190 (1960); 50, 24, 29 (1961); Mukasa et al., Biochim. Biophys. Acta 168, 132 (1968); Matsunaga, Nosoh, ibid. 215, 280 (1970); of human: Kasper, Deutsch, J. Biol. Chem. 238, 2325 (1963); Jamieson, ibid. 240, 2019 (1965); Poillon, Bearn, Biochim. Biophys. Acta 127, 407 (1966); Simons, Bearn, ibid. 175, 260 (1969); Ryden, Eur. J. Biochem. 26, 380 (1972); T. G. Samsonidze et al., Int. J. Pept. Protein Res. 14, 161 (1979); V. N. Zaitsev et al., Kristallografiya 25, 174 (1980), C.A. 92, 210415q (1980). Human metabolism: Kekki et al., Nature 209, 1252 (1966). Reviews of biological role: E. Frieden, H. S. Hsieh, Adv. Exp. Med. Biol. 74, 505-529 (1976); J. M. C. Gutteridge, Ann. Clin. Biochem. 15, 293-296 (1978). Comprehensive review: S. H. Laurie, E. S. Mohammed, Coord. Chem. Rev. 33, 279-312 (1980).

Salutaridine CAS Registry Number: 1936-18-1

CAS Name: 5,6,8,14-Tetradehydro-4-hydroxy-3,6-dimethoxy-17-methylmorphinan-7-one
Additional Names: floripavine
Percent Composition: C 69.71%, H 6.47%, N 4.28%, O 19.55%
Literature References: Intermediate in morphine synthesis; naturally occurring in (+)-form. Isolated from various species of Croton and Papaver: Barton et al., J. Chem. Soc. 1965, 2423; Pfeifer, Kühn, Pharmazie 23, 267 (1968). Structure and identity with floripavine: Mndzhoyan et al., C.A. 68, 114787w (1968). Synthesis: T. Kametani et al., J. Chem. Soc. C 1969, 2030; G. Horvath, S. Makleit, Acta Chim. Acad. Sci. Hung. 106, 37 (1981); of racemate: T. Kametani et al., J. Chem. Soc. Perkin Trans. 1 1972, 1435; C. Szántay et al., J. Org. Chem. 47, 594 (1982); of racemate and (-)-form: W. Ludwig, H. J. Schafer, Angew. Chem. Int. Ed. 25, 1025 (1986). Review: Stuart, Chem. Rev. 1971, 47.

Adrenalone CAS Registry Number: 99-45-6 肾上腺酮

CAS Name: 1-(3,4-Dihydroxyphenyl)-2-(methylamino)ethanone
Additional Names: 3',4'-dihydroxy-2-(methylamino)acetophenone; 3,4-dihydroxy-a-methylaminoacetophenone; adrenone; 4-methylaminocetopyro...
Literature References: Intermediate in some epinephrine manuf processes. Prepd from 4-chloroacetylpyrocatechol and methylamine: DE 152814 (Hoechst); Stolz, Ber. 37, 4152 (1904); by heating a-(p-toluene sulfonylmethylamino)-3,4-dimethoxyacetophenone with HCl under pressure: DE 277540 (Bayer); Frdl. 12, 764; Chem. Zentralbl. 1914, II, 740.

Pseudoionone CAS Registry Number: 141-10-6 6,10-二甲基-3,5,9-十一三烯-2-酮

CAS Name: 6,10-Dimethyl-3,5,9-undecatriene-2-one
Additional Names: citrylideneacetone; 2,6-dimethylhendeca-2,6,8-trien-10-one
Percent Composition: C 81.20%, H 10.48%, O 8.32%
Literature References: Intermediate in the synthesis of a- and b-ionone. Prepn from citral and acetone: Tiemann, Krüger, Ber. 26, 2692 (1893); Stiehl, J. Prakt. Chem. [2] 58, 84 (1898); Tiemann, Ber. 32, 115 (1899); Hibbert, Cannon, J. Am. Chem. Soc. 46, 119 (1924); A. Russel, R. L. Kenyon, Org. Synth. coll. vol. III, 747 (1955). A less pure product is obtained by the treatment of oil of lemon grass and acetone with bleaching powder, cobalt nitrate, and alcohol: Ziegler, J. Prakt. Chem. [2] 57, 493 (1898); Tiemann, Ber. 31, 2313 (1898); Haarmann, Reimer Co., DE 73089; Frdl. 3, 889. Synthesis: T. Onishi et al., Synthesis 1980, 651.

Prelog-Djerassi Lactone CAS Registry Number: 69056-12-8 (2R)-2-[(2S,3S,5R)-3,5-二甲基-6-氧基四氢-2H-吡喃-2-基]丙烷酸

CAS Name: (aR,2S,3S,5R)-Tetrahydro-a,3,5-trimethyl-6-oxo-2H-pyran-2-acetic acid
Additional Names: (+)-Prelog-Djerassi lactonic acid; 6-(1-carboxyethyl)-3,4,5,6-tetrahydro-3,5-dimethyl-2-pyranon...
Literature References: Intermediate in the synthesis of macrolide antibiotics. Isoln as degradation product of narbomycin, q.v.: R. Anliker et al., Helv. Chim. Acta 39, 1785 (1956); of methymycin, q.v.: C. Djerassi, J. A. Zderic, J. Am. Chem. Soc. 78, 6390 (1956). Abs config: R. W. Rickards, R. M. Smith, Tetrahedron Lett. 1970, 1025. Synthesis: P. A. Grieco et al., J. Am. Chem. Soc. 101, 4749 (1979); D. A. Evans, J. Bartroli, Tetrahedron Lett. 23, 807 (1982). Synthesis of (±)-form: S. Masamune et al., J. Am. Chem. Soc. 97, 3512 (1975); C. Santelli-Rouvier et al., Tetrahedron Lett. 35, 6101 (1994). Review of stereoselective syntheses: S. F. Martin, D. E. Guinn, Synthesis 1991, 245.

Oxenin CAS Registry Number: 3230-75-9 (8E,13cis)-10-羟基-11,12-二代水-7,10-二氢视黄醇

CAS Name: 11,12-Didehydro-7,10-dihydro-10-hydroxyretinol
Additional Names: 3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)nona-2,7-dien-4-yne-1,6-diol
Percent Composition: C 79.42%, H 10....
Literature References: Intermediate in the vitamin A synthesis. Prepn: Isler et al., Helv. Chim. Acta 30, 1911 (1947); Isler, US 2451739 (1948 to Hoffmann-La Roche); Kardys, US 3046310 (1962 to Pfizer).

Croscarmellose Sodium CAS Registry Number: 74811-65-7 交联羧甲基纤维素钠

Trademarks: Ac-Di-Sol (FMC)
Literature References: Internally cross-linked form of carboxymethylcellulose sodium (NaCMC), q.v. Prepd by lowering pH of NaCMC in solution, then heating: Technical Literature, FMC Corp. Use as tablet disintegrant: D. Gissinger, A. Stamm, Pharm. Ind. 42, 189 (1980); M. E. Sangalli et al., Boll. Chim. Farm. 128, 242 (1989). Evaluation of drug-excipient interaction: R. G. Hollenbeck et al., J. Pharm. Sci. 72, 325 (1983). Water sorption and thermal behavior: D. Faroongsarng, G. E. Peck, Drug Dev. Ind. Pharm. 20, 779 (1994). Mechanism of action study: R. Thibert, B. C. Hancock, J. Pharm. Sci. 85, 1255 (1996).

Fasudil CAS Registry Number: 103745-39-7 法舒地尔

CAS Name: Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine
Additional Names: N-(5-isoquinolinesulfonyl)-1,4-perhydrodiazepine; 1-(5-isoquinolinesulfonyl)homopiperazine
Percent Composit...
Literature References: Intracellular calcium antagonist. Prepn: H. Hidaka, T. Sone, EP 187371; eidem, US 4678783 (1986, 1987 both to Asahi); A. Morikawa et al., Chem. Pharm. Bull. 40, 770 (1992). Pharmacology: T. Asano et al., Br. J. Pharmacol. 98, 1091 (1989). Mechanism of action: idem et al., J. Pharmacol. Exp. Ther. 241, 1033 (1987). Clinical trials: M. Shibuya et al., J. Neurosurg. 76, 571 (1992). Acute toxicity: H. Koga et al., Yakuri to Chiryo 20, S1433 (1992), C.A. 117, 226005b (1992). Review of pharmacology and clinical evaluation: M. Shirotani et al., Cardiovasc. Drug Rev. 10, 333-357 (1992).