CAS: 66892-34-0; 6-Fluorochroman-4-One

上下游产品

3-Chloro-1-(5-Fluoro-2-Hydroxyphenyl)Propan-1-One 104147-77-5
6-Fluoro-4-Methylenechroman
5-氟-2-羟基苯乙酮 1-(5-Fluoro-2-Hydroxyphenyl)Ethan-1-One 394-32-1

3-(4-氟苯氧基)丙酸置于ppa体系中,化学反应 0.33H,以83%的收率获得产物6-氟-4-二氢色原酮
参考文献:醛糖还原酶抑制剂山梨醇的合成,绝对构型和构象.
标题:醛糖还原酶抑制剂山梨醇的合成,绝对构型和构象.
摘要:醛糖还原酶抑制剂2,3-二氢-6-氟螺[4H-1-苯并吡喃-4,4'-咪唑烷]-2',5'-二酮被拆分为其对映体.sorbinil,S异构体,在体内外比相应的r异构体是更好的酶抑制剂.介绍了用于确定其绝对构型的山梨醇x射线数据.溶液中山梨醇的NMR研究表明,存在两个构象异构体,它们具有较低的能量转换障碍.
DOI:10.1021/jm00149A030

专利信息

专利号:US-4431828-A
优先权日:1982-11-10
标题 :Regeneration of 6-fluoro-4-chromanone from by-products in the synthesis of sorbinil
发明人：CUE JR BERKELEY W; HAMMEN PHILIP D; MASSETT STEPHEN S
权利人:PFIZER
摘要:6-Fluoro-4-chromanone, a sorbinil intermediate, is regenerated from enantiomeric and mixtures of enantiomeric and racemic compounds obtained as major by-products in the synthesis of sorbinil. The regenerated intermediate is useful in the synthesis of additional sorbinil.

专利号:US-4286098-A
优先权日:1980-03-28
标 题:Process for the preparation of chiral hydantoins
发明人：SARGES REINHARD
权利人:PFIZER
摘要:A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. n The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.

专利号:US-4348526-A
优先权日:1980-03-28
标题:Intermediates in the preparation of chiral hydantoins
发明人：SARGES REINHARD
权利人:PFIZER
摘要:A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. n The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.

专利号:US-7405310-B2
优先权日:2001-03-05
标 题:Non-nucleoside reverse transcriptase inhibitors
发明人：LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA
权利人:MEDIVIR AB
摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.

专利号:US-4419521-A
优先权日:1981-11-12
标 题 :6-Halo-4-chromanamines useful as intermediates to make chiral hydantoins
发明人：SARGES REINHARD
权利人:PFIZER
摘要:A novel process for the synthesis of chiral hydantoins of the structure (I) wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure (II) is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure (III) addition of hydrogen cyanide to form the nitrile of structure (IV) condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure (V) and finally solvolysis of the latter to the chiral hydantoin of structure I.

专利号:US-6316437-B1
优先权日:1999-09-30
标题:Spirohydantoin compounds and uses thereof
发明人：HOFFMAN JACOB M
权利人:MERCK & CO INC
摘要:Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.