1,192,011. Naphthylcyclopentanes. BEECHAM GROUP Ltd. 19 May, 1967 [24 May, 1966; 27 April, 1967], Nos. 23113/66 and 19348/67. Heading C2C. The invention comprises d, l and dl compounds of formula wherein R is C 1-6 alkyl; R 1 is H, alkyl or dialkylaminoalkyl; R 2 is carboxy, alkoxycarbonyl, dialkylaminoalkoxycarbonyl, hydroxymethyl, methoxymethyl or acyloxymethyl; Z is optionally thioketalized CO, CHOH, CHOAcyl, CHOCH 3 , C(OH)C: CH or C: NOH; Y is CH 2 , CO, C: NOH, C: CHOH, C: CHSR 3 or C: CHNR 4 R 5 (where R 3 is alkyl and R 4 and R 5 are each alkyl or aryl); and lactones of those compounds wherein R 2 is carboxy and Z is CHOH; and acid-addition salts of those compounds having basic groups. These compounds are prepared by alkylating compounds of formula wherein X is a protecting group (e.g. benzylidene, furfurylidene, CHSR 3 or CHNR 4 R 5 ) to introduce the group R, converting the group CX in the resulting product to a group Y (when it is not already such a group) and, when required converting the 1-keto group to other groups Z. Many product interconversions are described and exemplified. dl - 5 - (N - methyl - anilinomethylene) - 3 - (6 - methoxy - 2 - naphthyl) - cyclopentanone - 2 - acetic acid and its methyl ester are prepared from dl-methyl 3 - (6 - methoxy - 2 - naphthyl) - cyclopentanone - 2 - acetate via dl - 5 - hydroxymethylene - 3 - (6 - methoxy - 2 - naphthyl) cyclopentanone - 2 - acetic acid. Said methyl ester is also obtainable from the parent acid.
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机译:1,192,011。萘环戊烷。 BEECHAM GROUP Ltd. 1967年5月19日[1966年5月24日; 1967年4月27日],第23113/66和19348/67号。标题C2C。本发明包括下式的d,l和dl化合物:其中R是C 1-6烷基; R 1为H,烷基或二烷基氨基烷基; R 2是羧基,烷氧基羰基,二烷基氨基烷氧基羰基,羟甲基,甲氧基甲基或酰氧基甲基; Z任选为硫代缩酮化的CO,CHOH,CHO酰基,CHOCH 3,C(OH)C:CH或C:NOH; Y为CH 2,CO,C:NOH,C:CHOH,C:CHSR 3或C:CHNR 4 R 5(其中R 3为烷基,R 4和R 5分别为烷基或芳基); R 2为羧基,Z为CHOH的那些化合物的内酯。那些具有碱性基团的化合物的酸加成盐。这些化合物是通过烷基化其中X为保护基的化学式(例如亚苄基,糠叉基,CHSR 3或CHNR 4 R 5)的烷基来制备的,以引入基团R,将所得产物中的CX基团转化为基团Y(当它(还不是这样的基团),并且在需要时将1-酮基转化为其他基团Z。描述并举例说明了许多产物互变。 dl-5-(N-甲基-苯氨基亚甲基)-3-(6-甲氧基-2-萘基)-环戊酮-2-乙酸及其甲酯是由dl-甲基3-(6-甲氧基-2-萘基)制备的)-环戊酮-2-乙酸酯通过dl-5-羟亚甲基-3-(6-甲氧基-2-萘基)环戊酮-2-乙酸。所述甲酯也可从母体酸获得。
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